This is a prospective, 12-week, open-label, single-arm study. The study population comprises individuals with refractory skin disease characteristic of dermatomyositis with no to minimal muscle involvement. After an up to 8-week Screening Period, eligible participants will receive brepocitinib 30 mg orally (PO) QD for 12 weeks.

Start Date01 Jun 2024

Sponsor / Collaborator

Priovant Therapeutics, Inc.

NCT05523765 / Active, not recruitingPhase 2

A Phase 2 Randomized, Double-Masked, Dose-Ranging Study to Investigate the Safety and Efficacy of Oral Brepocitinib in Adults With Active Non-Infectious Intermediate-, Posterior-, and Panuveitis

This study will evaluate the clinical safety and efficacy of oral brepocitinib in participants with active intermediate, posterior, or pan non-infectious uveitis (NIU).

Start Date14 Nov 2022

Sponsor / Collaborator

Priovant Therapeutics, Inc.

NCT05437263 / RecruitingPhase 3

A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Efficacy and Safety of Oral Brepocitinib in Adults With Dermatomyositis

This is a phase 3, multicenter, randomized, placebo-controlled, double-blind study of treatment with brepocitinib (TYK2/JAK1 inhibitor) in adults with dermatomyositis (DM). The primary objective of this study is to assess the efficacy of two dose levels of brepocitinib in comparison to placebo, as measured by differences in the Total Improvement Score (TIS). After 52 weeks of double-blind treatment, participants have the option to continue therapy in a 52 week open-label extension phase where all participants will receive brepocitinib.

Start Date31 Oct 2022

Sponsor / Collaborator

Priovant Therapeutics, Inc.

100 Clinical Results associated with Brepocitinib

100 Translational Medicine associated with Brepocitinib

100 Patents (Medical) associated with Brepocitinib

Literatures (Medical) associated with Brepocitinib

17 Jun 2024·Drug metabolism and disposition: the biological fate of chemicals

The Metabolism and Disposition of Brepocitinib in Humans and Characterization of the Formation Mechanism of an Aminopyridine Metabolite.

Article

Author: Walker, Gregory S ; Doran, Angela ; Qiu, Ruolun ; Sharma, Raman ; Balesano, Amanda ; Wright, Stephen W ; Dowty, Martin E ; Dantonio, Alyssa ; Niosi, Mark

Brepocitinib is an oral once-daily Janus kinase 1 and Tyrosine kinase 2 selective inhibitor currently in development for the treatment of several autoimmune disorders. Mass balance and metabolic profiles were determined using accelerator mass spectrometry in six healthy male participants following a single oral 60 mg dose of ¹⁴C-brepocitinib (∼300 nCi). The average mass balance recovery was 96.7% ± 6.3%, with the majority of dose (88.0% ± 8.0%) recovered in urine and 8.7% ± 2.1% of the dose recovered in feces. Absorption of brepocitinib was rapid, with maximal plasma concentrations of total radioactivity and brepocitinib achieved within 0.5 hours after dosing. Circulating radioactivity consisted primarily of brepocitinib (47.8%) and metabolite M1 (37.1%) derived from hydroxylation at the C5' position of the pyrazole ring. Fractional contributions to metabolism via cytochrome P450 enzymes were determined to be 0.77 for CYP3A4/5 and 0.14 for CYP1A2 based on phenotyping studies in human liver microsomes. However, additional clinical studies are required to understand the potential contribution of CYP1A1. Approximately 83% of the dose was eliminated as N-methylpyrazolyl oxidative metabolites, with 52.1% of the dose excreted as M1 alone. Notably, M1 was not observed as a circulating metabolite in earlier metabolic profiling of human plasma from a multiple ascending dose study with unlabeled brepocitinib. Mechanistic studies revealed that M1 was highly unstable in human plasma and phosphate buffer, undergoing chemical oxidation leading to loss of the 5-hydroxy-1-methylpyrazole moiety and formation of aminopyrimidine cleavage product M2. Time-dependent inhibition and trapping studies with M1 yielded insights into the mechanism of this unusual and unexpected instability. SIGNIFICANCE STATEMENT: This study provides a detailed understanding of the disposition and metabolism of brepocitinib, a JAK1/TYK2 inhibitor for atopic dermatitis, in humans as well as characterization of clearance pathways and pharmacokinetics of brepocitinib and its metabolites.

24 May 2024·Journal of clinical medicine

Therapeutic Potential of Targeting the JAK/STAT Pathway in Psoriasis: Focus on TYK2 Inhibition.

Review

Author: Tognetti, Linda ; Rubegni, Pietro ; Dragotto, Martina ; Calabrese, Laura ; D'Onghia, Martina ; Trovato, Emanuele

Psoriasis is an inflammatory skin disease with a chronic relapsing course and an often-detrimental impact on patients' quality of life. Thanks to incredible advances in research over the past few decades, the therapeutic armamentarium of psoriasis is now reasonably broad and structured, with several therapeutic agents that have demonstrated successful long-term control of this condition. However, there are still unfulfilled gaps resulting from the inherent limitations of existing therapies, which have paved the way for the identification of new therapeutic strategies or the improvement of existing ones. A great deal of attention has recently been paid to the JAK/STAT pathway, playing a crucial role in chronic inflammatory skin diseases, including psoriasis. Indeed, in a disease with such a complex pathogenesis, the possibility to antagonize multiple molecular pathways via JAK/STAT inhibition offers an undeniable therapeutic advantage. However, data from clinical trials evaluating the use of oral JAK inhibitors in immune-mediated disorders, such as RA, have arisen safety concerns, suggesting a potentially increased risk of class-specific AEs such as infections, venous thromboembolism, and malignancies. New molecules are currently under investigation for the treatment of psoriasis, such as deucravacitinib, an oral selective inhibitor that binds to the regulatory domain of TYK2, brepocitinib (PF-06700841) and PF-06826647 that bind to the active site in the catalytic domain. Due to the selective TYK2 blockade allowing the inhibition of key cytokine-mediated signals, such as those induced by IL-12 and IL-23, anti-TYK2 agents appear to be very promising as the safety profile seems to be superior compared with pan-JAK inhibitors. The aim of our review is to thoroughly explore the rationale behind the usage of JAK inhibitors in PsO, their efficacy and safety profiles, with a special focus on oral TYK2 inhibitors, as well as to provide a forward-looking update on novel therapeutic strategies targeting the TYK2 pathway in psoriasis.

23 May 2024·Italian journal of dermatology and venereology

Exploring Janus kinase inhibitors for alopecia areata: a comprehensive review.

Article

Author: Srivastava, Gautam ; Bushwereb, Randa

INTRODUCTIONAlopecia areata poses a significant challenge due to its chronic autoimmune nature, leading to psychosocial impacts. Recent strides in understanding the disease have spotlighted Janus kinase (JAK) inhibitors as potential therapies. This comprehensive review aims to assess Baricitinib's efficacy and safety in treating scalp, eyebrow, and eyelash alopecia areata, and compare the effectiveness of Ritlecitinib and Brepocitinib.EVIDENCE ACQUISITIONConducting a thorough electronic literature search, we focused on clinical studies of JAK inhibitors for moderate to severe alopecia areata from 2015 onward. Key databases, including MEDLINE, PubMed, Cochrane Library, EMBASE, Google Scholar, and Medscape, were utilized. Primary outcomes included changes in the Severity of Alopecia Tool (SALT) score, with safety data evaluating adverse events and serious adverse events. The risk of bias was assessed using the Cochrane Risk of Bias Tool.EVIDENCE SYNTHESISAmong the twelve studies identified, Baricitinib demonstrated superior efficacy over placebo at 24 weeks, with both 2mg and 4mg dosages significantly reducing SALT scores. Comparative efficacy at 24 weeks for Baricitinib, Brepocitinib, and Ritlecitinib showed similar effectiveness compared to placebo, with a marginal superiority observed for Baricitinib 4mg. All JAK inhibitors were well-tolerated, with reported adverse events primarily being mild and manageable.CONCLUSIONSCollectively, the reviewed studies affirm JAK inhibitors, particularly Baricitinib, as promising treatments for moderate to severe alopecia areata. These inhibitors exhibit superior efficacy, as indicated by notable reductions in SALT scores, and are well-tolerated, with predominantly mild and manageable adverse events.

News (Medical) associated with Brepocitinib

30 May 2024

·www.globenewswire.com

Roivant Reports Financial Results for the Fourth Quarter and Fiscal Year Ended March 31, 2024, and Provides Business Update

BASEL, Switzerland and LONDON and NEW YORK, May 30, 2024 (GLOBE NEWSWIRE) -- Roivant (Nasdaq: ROIV) today reported its financial results for the fourth quarter and fiscal year ended March 31, 2024, and provided a business update. Once-daily brepocitinib produced the best Treatment Failure rates observed to date among studies in active non-infectious uveitis (NIU), supporting initiation of a pivotal program in NIU in the second half of calendar year 2024Brepocitinib is well positioned to support a potential multi-blockbuster franchise in rare and orphan autoimmune disease with an ongoing pivotal study in dermatomyositis on track to read out in calendar year 2025Following a recently completed Type B meeting with the FDA, Immunovant is on track to initiate 4-5 potentially registrational studies with IMVT-1402 over the fiscal year ending March 31, 2025Immunovant expects to announce detailed results from the study of batoclimab in Graves’ disease (GD) as well as an overview of the development plan of IMVT-1402 in GD in the fall of 2024VTAMA® sNDA submission for atopic dermatitis was accepted by the FDA; PDUFA action is expected in the fourth quarter of calendar year 2024, potentially enabling a four-fold market expansionVTAMA, approved for psoriasis, net product revenue was $75.1M for the fiscal year ended March 31, 2024, with over 385,000 prescriptions written by over 15,300 unique prescribers since launchRoivant renegotiated Dermavant’s debt obligations, reducing potential cash payments due by over $300M in the aggregate. Approximately $225M of this reduction is expected to be achieved over the next three fiscal yearsRoivant has $852M in share repurchase authorization available following the repurchase of Sumitomo’s entire stake at $9.10 per share for $648M, which reduced outstanding shares by 9%Net cash used in operating activities for the quarter was $108MRoivant reported its consolidated cash, cash equivalents and restricted cash of $6.6B at March 31, 2024, supporting cash runway into profitability “We finished our fiscal year with yet another productive quarter for the company,” said Matt Gline, CEO of Roivant. “The Priovant team announced outstanding data for patients with NIU, reaffirming our view on the blockbuster potential of brepocitinib, which we expect will continue to deliver benefit to patients with unmet need. Our board has approved a significant buyback program, allowing us to return capital to shareholders and to increase exposure to our most exciting current and future programs. I could not be more excited for what we’ve accomplished and what I believe we will deliver in our next chapter ahead.” Recent Developments Priovant: In April 2024, Priovant announced positive results from the Phase 2 study (NEPTUNE) evaluating brepocitinib in non-anterior non-infectious uveitis. On the pre-specified primary efficacy endpoint of Treatment Failure at week 24, 29% of subjects receiving brepocitinib 45 mg and 44% of subjects receiving brepocitinib 15 mg met Treatment Failure criteria (lower failure rates reflect greater treatment benefit). The brepocitinib 45 mg results represent the best Treatment Failure rates observed to date among studies in active NIU measuring this registrational endpoint. All secondary efficacy endpoints were also positive and dose responsive, including measurements of potential benefit on prevention and treatment of uveitic macular edema. NEPTUNE represents the seventh positive Phase 2 study for brepocitinib with over 1,400 subjects and patients treated with brepocitinib in clinical trials. Brepocitinib was generally safe and well-tolerated in the study, with no new safety or tolerability signals identified.Immunovant: Following a recently completed Type B meeting with the FDA, 4-5 potentially registrational programs for IMVT-1402 are on track to be initiated by March 31, 2025. Immunovant is prioritizing the development of IMVT-1402 as the lead asset going forward.In March 2024, Immunovant was awarded U.S. Patent No. 11,926,669 covering composition of matter of IMVT-1402 and its binding sequence to FcRn, method of use of the antibody for treating autoimmune disease, and methods for its manufacturing. Not including any potential patent term extension, the issued composition-of-matter patent term will extend until June 2043. Dermavant: For the fourth quarter and fiscal year ended March 31, 2024, Roivant reported VTAMA net product revenue of $19.3M, and $75.1M, respectively. As of May 2024, over 385,000 VTAMA prescriptions have been written by over 15,300 unique prescribers for psoriasis. VTAMA is covered for over 138M US commercial lives, including coverage by all three of the top pharmacy benefit managers.In April 2024, Dermavant announced FDA acceptance of VTAMA’s sNDA submission for the treatment of atopic dermatitis in adults and children 2 years of age and older. PDUFA action is expected in the fourth quarter of calendar year 2024.In May 2024, Roivant renegotiated Dermavant’s debt obligations, reducing potential cash payments due by over $300M in the aggregate. Approximately $225M of this reduction is expected to be achieved over the next three fiscal years. Genevant: In April 2024, the U.S. District Court for the District of Delaware issued its claim construction (Markman) ruling in the lawsuit brought by Genevant and Arbutus against Moderna. The court agreed with Genevant and Arbutus’ proposed constructions for three of the four disputed terms.Kinevant: In April 2024, Kinevant completed enrollment in RESOLVE-LUNG, a Phase 2 study evaluating namilumab for chronic pulmonary sarcoidosis.Roivant: In April 2024, Roivant announced that its board of directors had authorized a share repurchase program for up to $1.5B of the company’s common shares. Pursuant to that program, the company completed the repurchase of all 71.3M shares held by Sumitomo Pharma at a purchase price of $9.10 per share. The aggregate purchase price for Sumitomo Pharma’s stake was approximately $648.4M, reducing Roivant’s shares outstanding by approximately 9%.Roivant reported its consolidated cash, cash equivalents and restricted cash of $6.6B at March 31, 2024. Giving effect to the Sumitomo share repurchase, Roivant’s cash, cash equivalents and restricted cash at March 31, 2024 would have been approximately $5.9B. Major Upcoming Milestones Dermavant expects PDUFA action for VTAMA in atopic dermatitis in the fourth quarter of calendar year 2024.Kinevant plans to report topline data from the ongoing Phase 2 trial of namilumab for the treatment of sarcoidosis in the fourth quarter of calendar year 2024.Priovant expects topline results from the ongoing Phase 3 trial of brepocitinib in dermatomyositis (DM) in calendar year 2025 and to initiate a Phase 3 pivotal trial of brepocitinib in the second half of calendar year 2024.Immunovant plans to have initiated 4-5 potentially registrational programs by March 31, 2025, and plans to have initiated studies in a total of 10 indications by March 31, 2026 for IMVT-1402. Detailed results from the batoclimab study in Graves’ Disease (GD) and an overview of the development plan of IMVT-1402 in GD are expected in the fall of 2024. Immunovant expects to report topline data from the study of batoclimab in MG over this fiscal year with further potentially registrational development of IMVT-1402 in MG expected to begin in the same timeframe. Immunovant has decided to run the study of batoclimab in CIDP longer prior to unblinding period 1 in order to better ensure that the data from the batoclimab study can be used to optimize development of IMVT-1402 in CIDP. Top-line data from the ongoing Phase 3 clinical trial in thyroid eye disease (TED) is expected in the first half of calendar year 2025. Fourth Quarter and Fiscal Year Ended March 31, 2024 Financial Summary Cash Position As of March 31, 2024, the company had cash, cash equivalents and restricted cash of approximately $6.6 billion. Research and Development Expenses Research and development (R&D) expenses decreased by $11.0 million to $120.9 million for the three months ended March 31, 2024, compared to $131.9 million for the three months ended March 31, 2023, primarily due to a decrease in program-specific costs of $25.8 million, partially offset by increases in share-based compensation of $5.9 million, other expenses of $4.6 million, and personnel-related expenses of $4.3 million. The decrease of $25.8 million in program-specific costs was primarily driven by a decrease of $19.8 million in other development and discovery programs, which in part resulted from the deconsolidation of Proteovant in August 2023 along with the reprioritization of certain programs and drug discovery efforts. The change also included a decrease of $5.9 million relating to RVT-3101 as a result of the sale of the rights to further develop and manufacture RVT-3101 to Roche in December 2023. Non-GAAP R&D expenses were $109.7 million for the three months ended March 31, 2024, compared to $126.0 million for the three months ended March 31, 2023. Research and development expenses decreased by $23.5 million to $501.7 million for the year ended March 31, 2024, compared to $525.2 million for the year ended March 31, 2023, primarily due to a decrease in program-specific costs of $42.4 million, partially offset by increases in other expenses of $10.7 million, personnel-related expenses of $4.5 million, and share-based compensation of $3.7 million. The decrease of $42.4 million in program-specific costs was primarily driven by a decrease of $83.1 million in other development and discovery program expense, which in part resulted from the deconsolidation of Proteovant in August 2023 along with the reprioritization of certain programs and drug discovery efforts. This decrease was partially offset by increases of $32.8 million relating to IMVT-1402 and $27.6 million relating to RVT-3101, which was acquired in November 2022. The rights to further develop and manufacture RVT-3101 were sold to Roche in December 2023. Non-GAAP R&D expenses were $462.6 million for the year ended March 31, 2024, compared to $489.2 million for the year ended March 31, 2023. Acquired In-Process Research and Development Expenses There was no acquired in-process research and development (IPR&D) expense for the three months ended March 31, 2024 and 2023. Acquired in-process research and development expenses decreased by $71.3 million to $26.5 million for the year ended March 31, 2024, compared to $97.7 million for the year ended March 31, 2023. The decrease was primarily due to higher consideration for the purchase of IPR&D during the year ended March 31, 2023 as a result of consideration for the purchase of IPR&D of $87.7 million relating to the acquisition of RVT-3101 in November 2022 and the achievement of a development milestone relating to batoclimab, which resulted in a one-time milestone expense of $10.0 million. Acquired in-process research and development expenses for the year ended March 31, 2024 was driven by $14.0 million of consideration for the purchase of IPR&D relating to an asset acquisition completed by a newly-formed subsidiary and $12.5 million relating to the achievement of development and regulatory milestones for batoclimab. Selling, General and Administrative Expenses Selling, general and administrative (SG&A) expenses increased by $44.1 million to $169.6 million for the three months ended March 31, 2024, compared to $125.5 million for the three months ended March 31, 2023. The increase was primarily due to an increase in share-based compensation of $15.6 million, an increase in SG&A expenses at Dermavant of $8.5 million due to the progression of the commercial launch of VTAMA, and an increase of $8.5 million resulting from a special one-time cash retention bonus award granted to employees. Non-GAAP SG&A expenses were $131.3 million for the three months ended March 31, 2024, compared to $102.6 million for the three months ended March 31, 2023. Selling, general and administrative expenses increased by $86.9 million to $687.4 million for the year ended March 31, 2024, compared to $600.5 million for the year ended March 31, 2023. The increase was primarily due to an increase in selling, general and administrative expenses of $55.7 million at Dermavant as a result of the progression of the commercial launch of VTAMA and an increase in personnel-related expenses of $25.1 million, primarily as a result of a special one-time cash retention bonus award granted to employees. Non-GAAP SG&A expenses were $514.8 million for the year ended March 31, 2024, compared to $407.6 million for the year ended March 31, 2023. A majority of the non-GAAP SG&A expenses of $514.8 million were related to Dermavant’s SG&A and ongoing VTAMA commercial launch activities. Gain on Sale of Telavant Net Assets Gain on sale of Telavant net assets was approximately $5.3 billion for the year ended March 31, 2024 and resulted from the sale of our entire equity interest in Telavant to Roche in December 2023. At closing, we received approximately $5.2 billion in cash for our pro rata portion of the consideration. Additionally, we derecognized the carrying amount of noncontrolling interest in Telavant of $87.5 million and transferred net liabilities of $26.5 million. This resulted in a gain of approximately $5.3 billion. Income (Loss) from Continuing Operations Loss from continuing operations was $182.5 million for the three months ended March 31, 2024, compared to $175.4 million for the three months ended March 31, 2023. On a per common share basis, loss from continuing operations was $0.19 and $0.20 for the three months ended March 31, 2024 and 2023, respectively. Non-GAAP loss from continuing operations was $188.1 million for the three months ended March 31, 2024, compared to $189.4 million for the three months ended March 31, 2023. Income from continuing operations was approximately $4.2 billion for the year ended March 31, 2024, compared to a loss from continuing operations of $1.2 billion for the year ended March 31, 2023. On a basic and diluted per common share basis, income from continuing operations was $5.55 and $5.23, respectively, for the year ended March 31, 2024. On a per common share basis, loss from continuing operations was $1.58 for the year ended March 31, 2023. Non-GAAP loss from continuing operations was $799.9 million for the year ended March 31, 2024, compared to $924.3 million for the year ended March 31, 2023. ROIVANT SCIENCES LTD.Selected Balance Sheet Data(in thousands) March 31, 2024 March 31, 2023 Cash, cash equivalents and restricted cash$6,550,450 $1,692,115Total assets 7,222,482 2,389,604Total liabilities 773,953 782,017Total shareholders’ equity 6,448,529 1,607,587Total liabilities and shareholders’ equity 7,222,482 2,389,604 ROIVANT SCIENCES LTD.Consolidated Statements of Operations(in thousands, except share and per share amounts) Three Months Ended March 31, Years Ended March 31, 2024 2023 2024 2023 (Unaudited) (Unaudited) Revenues: Product revenue, net$19,308 $13,657 $75,057 $28,011 License, milestone and other revenue 9,622 13,719 49,738 33,269 Revenue, net 28,930 27,376 124,795 61,280 Operating expenses: Cost of revenues 4,412 4,175 15,560 13,128 Research and development (includes $10,290 and $4,366 of share-based compensation expense for the three months ended March 31, 2024 and 2023, respectively, and $34,595 and $30,914 of share-based compensation expense for the years ended March 31, 2024 and 2023, respectively) 120,902 131,857 501,736 525,215 Acquired in-process research and development — — 26,450 97,749 Selling, general and administrative (includes $36,396 and $20,832 of share-based compensation expense for the three months ended March 31, 2024 and 2023, respectively, and $164,841 and $186,603 of share-based compensation expense for the years ended March 31, 2024 and 2023, respectively) 169,616 125,510 687,443 600,506 Total operating expenses 294,930 261,542 1,231,189 1,236,598 Gain on sale of Telavant net assets — — 5,348,410 — (Loss) income from operations (266,000) (234,166) 4,242,016 (1,175,318) Change in fair value of investments (15,907) (32,462) 47,973 20,815 Change in fair value of debt and liability instruments (6,433) (12,031) 78,943 78,001 Gain on deconsolidation of subsidiaries (15,418) — (32,772) (29,276)Interest income (83,458) (14,284) (146,425) (32,184)Interest expense 7,175 8,575 34,778 27,968 Other expense (income), net 39,494 (4,748) 6,089 (15,808)(Loss) income from continuing operations before income taxes (191,453) (179,216) 4,253,430 (1,224,834)Income tax (benefit) expense (8,957) (3,793) 22,224 5,190 (Loss) income from continuing operations, net of tax (182,496) (175,423) 4,231,206 (1,230,024)Income from discontinued operations, net of tax — 114,561 — 114,561 Net (loss) income (182,496) (60,862) 4,231,206 (1,115,463)Net loss attributable to noncontrolling interests (31,381) (27,245) (117,720) (106,433)Net (loss) income attributable to Roivant Sciences Ltd.$(151,115) $(33,617) $4,348,926 $(1,009,030) Amounts attributable to Roivant Sciences Ltd.: (Loss) income from continuing operations, net of tax$(151,115) $(148,178) $4,348,926 $(1,123,591)Income from discontinued operations, net of tax — 114,561 — 114,561 Net (loss) income attributable to Roivant Sciences Ltd.$(151,115) $(33,617) $4,348,926 $(1,009,030) Net (loss) income per common share, basic: (Loss) income from continuing operations$(0.19) $(0.20) $5.55 $(1.58)Income from discontinued operations, net of tax$— $0.15 $— $0.16 Net (loss) income$(0.19) $(0.05) $5.55 $(1.42)Net (loss) income per common share, diluted: (Loss) income from continuing operations$(0.19) $(0.20) $5.23 $(1.58)Income from discontinued operations, net of tax$— $0.15 $— $0.16 Net (loss) income$(0.19) $(0.05) $5.23 $(1.42)Weighted average shares outstanding: Basic 802,859,062 742,541,052 783,248,906 712,791,115 Diluted 802,859,062 742,541,052 831,049,444 712,791,115 ROIVANT SCIENCES LTD.Reconciliation of GAAP to Non-GAAP Financial Measures(unaudited, in thousands) Three Months Ended March 31, Years Ended March 31, Note 2024 2023 2024 2023 (Loss) income from continuing operations, net of tax $(182,496) $(175,423) $4,231,206 $(1,230,024)Adjustments: Cost of revenues: Amortization of intangibles(1) 2,421 2,298 9,632 7,468 Share-based compensation(2) 38 37 191 95 Research and development: Share-based compensation(2) 10,290 4,366 34,595 30,914 Depreciation and amortization(3) 873 1,539 4,590 5,097 Selling, general and administrative: Share-based compensation(2) 36,396 20,832 164,841 186,603 Depreciation and amortization(3) 1,912 2,116 7,814 6,292 Gain on sale of Telavant net assets(4) — — (5,348,410) — Other: Change in fair value of investments(5) (15,907) (32,462) 47,973 20,815 Change in fair value of debt and liability instruments(6) (6,433) (12,031) 78,943 78,001 Gain on deconsolidation of subsidiaries(7) (15,418) — (32,772) (29,276)Estimated income tax impact from adjustments(8) (19,813) (704) 1,538 (294) Adjusted loss from continuing operations, net of tax (Non-GAAP) $(188,137) $(189,432) $(799,859) $(924,309) Three Months Ended March 31, Years Ended March 31, Note 2024 2023 2024 2023 Research and development expenses $120,902 $131,857 $501,736 $525,215 Adjustments: Share-based compensation(2) 10,290 4,366 34,595 30,914 Depreciation and amortization(3) 873 1,539 4,590 5,097 Adjusted research and development expenses (Non-GAAP) $109,739 $125,952 $462,551 $489,204 Three Months Ended March 31, Years Ended March 31, Note 2024 2023 2024 2023 Selling, general and administrative expenses $169,616 $125,510 $687,443 $600,506 Adjustments: Share-based compensation(2) 36,396 20,832 164,841 186,603 Depreciation and amortization(3) 1,912 2,116 7,814 6,292 Adjusted selling, general and administrative expenses (Non-GAAP) $131,308 $102,562 $514,788 $407,611 Notes to non-GAAP financial measures: (1) Represents non-cash amortization of intangible assets associated with milestone payments made in connection with regulatory approvals. (2) Represents non-cash share-based compensation expense. (3) Represents non-cash depreciation and amortization expense, other than amortization of intangible assets associated with milestone payments made in connection with regulatory approvals. (4) Represents a one-time gain on the sale of Telavant net assets to Roche in December 2023. (5) Represents the unrealized (gain) loss on equity investments in unconsolidated entities that are accounted for at fair value with changes in value reported in earnings. (6) Represents the change in fair value of debt and liability instruments, which is non-cash and primarily includes the unrealized loss relating to the measurement and recognition of fair value on a recurring basis of certain liabilities. (7) Represents the one-time gain on deconsolidation of subsidiaries. (8) Represents the estimated tax effect of the adjustments. Roivant will also present at two additional upcoming investor conferences: Fireside Chat at Jefferies Global Healthcare Conference in New York at 11:30 a.m. ET on June 5, 2024Fireside Chat at Goldman Sachs 45th Annual Global Healthcare Conference in Miami at 8:40 a.m. ET on June 10, 2024 Investor Conference Call InformationRoivant will host a live conference call and webcast at 8:00 a.m. ET on Thursday, May 30, 2024, to report its financial results for the fourth quarter and fiscal year ended March 31, 2024, and provide a corporate update. To access the conference call by phone, please register online using this registration link. The presentation and webcast details will also be available under “Events & Presentations” in the Investors section of the Roivant website at https://investor.roivant.com/news-events/events. The archived webcast will be available on Roivant’s website after the conference call. About Roivant Roivant is a commercial-stage biopharmaceutical company that aims to improve the lives of patients by accelerating the development and commercialization of medicines that matter. Today, Roivant’s pipeline includes VTAMA, a novel topical approved for the treatment of psoriasis and in development for the treatment of atopic dermatitis; IMVT-1402 and batoclimab, fully human monoclonal antibodies targeting the neonatal Fc receptor (“FcRn”) in development across several IgG-mediated autoimmune indications; and brepocitinib, a potent small molecule inhibitor of TYK2 and JAK1 for the treatment of dermatomyositis and non-infectious uveitis, in addition to other clinical stage molecules. We advance our pipeline by creating nimble subsidiaries or “Vants” to develop and commercialize our medicines and technologies. Beyond therapeutics, Roivant also incubates discovery-stage companies and health technology startups complementary to its biopharmaceutical business. For more information, www.roivant.com. Roivant Forward-Looking Statements This press release contains forward-looking statements. Statements in this press release may include statements that are not historical facts and are considered forward-looking within the meaning of Section 27A of the Securities Act of 1933, as amended (the “Securities Act”), and Section 21E of the Securities Exchange Act of 1934, as amended (the “Exchange Act”), which are usually identified by the use of words such as “anticipate,” “believe,” “continue,” “could,” “estimate,” “expect,” “intends,” “may,” “might,” “plan,” “possible,” “potential,” “predict,” “project,” “should,” “would” and variations of such words or similar expressions. The words may identify forward-looking statements, but the absence of these words does not mean that a statement is not forward-looking. We intend these forward-looking statements to be covered by the safe harbor provisions for forward-looking statements contained in Section 27A of the Securities Act and Section 21E of the Exchange Act. Our forward-looking statements include, but are not limited to, statements regarding our or our management team’s expectations, hopes, beliefs, intentions or strategies regarding the future, and statements that are not historical facts, including statements about potential share repurchases, the clinical and therapeutic potential of our products and product candidates, the availability and success of topline results from our ongoing clinical trials, any commercial potential of our products and product candidates and the benefits expected to be realized from Dermavant’s renegotiation of its existing debt obligations. In addition, any statements that refer to projections, forecasts or other characterizations of future events or circumstances, including any underlying assumptions, are forward-looking statements. Although we believe that our plans, intentions, expectations and strategies as reflected in or suggested by those forward-looking statements are reasonable, we can give no assurance that the plans, intentions, expectations or strategies will be attained or achieved. Furthermore, actual results may differ materially from those described in the forward-looking statements and will be affected by a number of risks, uncertainties and assumptions, including, but not limited to, those risks set forth in the Risk Factors section of our filings with the U.S. Securities and Exchange Commission. Moreover, we operate in a very competitive and rapidly changing environment in which new risks emerge from time to time. These forward-looking statements are based upon the current expectations and beliefs of our management as of the date of this press release and are subject to certain risks and uncertainties that could cause actual results to differ materially from those described in the forward-looking statements. Except as required by applicable law, we assume no obligation to update publicly any forward-looking statements, whether as a result of new information, future events or otherwise. Contacts:InvestorsRoivant Investor Relationsir@roivant.com MediaStephanie LeeRoivant Sciencesstephanie.lee@roivant.com

Phase 2Clinical ResultDrug ApprovalPhase 3Financial Statement

25 Apr 2024

·www.biospace.com

Roivant and Kinevant Sciences Complete Enrollment in RESOLVE-Lung, a Phase 2 Study Evaluating Namilumab for Chronic Pulmonary Sarcoidosis

Namilumab is a fully human monoclonal antibody that inhibits granulocyte-macrophage colony-stimulating factor (GM-CSF), a pro-inflammatory cytokine believed to play a key role in the pathogenesis of sarcoidosis RESOLVE-Lung is a randomized, double-blind, placebo-controlled Phase 2 study designed to be supportive of registration that enrolled 107 pulmonary sarcoidosis patients whose disease is not well-controlled despite currently available treatments Topline results are expected by the end of calendar year 2024 BASEL, Switzerland & LONDON & NEW YORK--(BUSINESS WIRE)-- Roivant (Nasdaq: ROIV) and Kinevant Sciences, a clinical-stage biopharmaceutical company developing new medicines for rare inflammatory and autoimmune diseases, today announced the successful completion of enrollment in its Phase 2 study evaluating namilumab for the treatment of chronic pulmonary sarcoidosis (RESOLVE-Lung). Approximately 200,000 people in the U.S. (and more than 1 million worldwide) are estimated to have sarcoidosis, an immune-mediated inflammatory disease that can affect any organ in the body, with about 90% of cases involving the lung. Namilumab is a potent anti-GM-CSF monoclonal antibody formulated to be conveniently administered once-monthly as a subcutaneous injection that has the potential to be the first disease-modifying therapy for sarcoidosis. Potentially supportive of registration, RESOLVE-Lung is a randomized, double-blind, placebo-controlled Phase 2 study designed to enroll a minimum of 100 pulmonary sarcoidosis patients whose disease is not well-controlled despite currently available treatment options. “People living with pulmonary sarcoidosis clearly need new therapeutic options that can more safely and effectively control or resolve their disease,” said Bill Gerhart, CEO of Kinevant. “Completing enrollment for this study is an important milestone in our journey to develop a new therapy for those living with pulmonary sarcoidosis. I am grateful for the patients who volunteered to participate in the study, as well as for the extraordinary efforts of the Kinevant team, our industry partners, clinical trial site staff, and patient advocacy groups, all of whom came together to overcome the unique challenges of this disease to successfully enroll this study. We are very hopeful about the outcome, and we look forward to reporting topline results by the end of the year.” Pulmonary sarcoidosis is a lung disease characterized by the presence of granulomas (clumps of immune cells) of unknown etiology that can cause breathlessness, fatigue, and pain. The resulting inflammation, if not effectively treated, can result in lung tissue scarring (fibrosis), lung dysfunction, and eventually lung failure. Approximately 50% of diagnosed patients require chronic therapy to treat symptoms and prevent progression. Oral steroids (e.g., prednisone) and off-label immunosuppressive therapies (e.g., methotrexate) are first- and second-line therapies respectively for sarcoidosis; however, these therapeutic options are often not effective or can be accompanied by serious side effects. Evidence from non-clinical studies indicate that GM-CSF is a key cytokine driving granuloma formation and inflammation in sarcoidosis, and that inhibiting GM-CSF can reduce granuloma activity and the resulting inflammation, leading potentially to a reduction in symptoms and resolution of the underlying disease. Namilumab is a potent inhibitor of GM-CSF that has been observed to be generally safe and well-tolerated in more than 350 participants across multiple clinical trials. Thus, namilumab has the potential to be the only well-tolerated and effective therapy for sarcoidosis, as well as the first therapy approved specifically for pulmonary sarcoidosis. “Pulmonary sarcoidosis is a complex and challenging condition, with limited treatment options, and many unacceptable side effects. There is a need for new and better therapies to be developed,” said Mary McGowan, CEO of the Foundation for Sarcoidosis Research. “We are proud to have worked with Kinevant on the successful enrollment of this clinical trial. We are grateful to the sarcoidosis patient community who embraced this opportunity to lead us toward a potential new therapy as well as a deeper understanding of sarcoidosis.” About RESOLVE-Lung The RESOLVE-Lung study is a Phase 2 randomized, double-blind, placebo-controlled study of namilumab for the treatment of pulmonary sarcoidosis being conducted at multiple sites in the U.S. and Europe. The study has enrolled 107 pulmonary sarcoidosis patients considered not well-controlled despite available therapeutic options. Patients in the study receive a once-monthly subcutaneous injection of namilumab or placebo (following the initial dosing period) for approximately six months. The goal of the study is to assess the efficacy and safety of namilumab in patients with pulmonary sarcoidosis during the 6-month blinded treatment period. The primary endpoint is the difference in the proportion of patients with a rescue event due to worsening of their pulmonary sarcoidosis. Secondary endpoints include changes in pulmonary function, patient reported outcomes, steroid use, safety, and tolerability. All patients who complete the 26-week double-blind treatment period are eligible to participate in a 28-week open-label extension treatment period on namilumab. More information can be found at About Namilumab Namilumab is an investigational, fully human monoclonal antibody formulated to be conveniently administered once a month as a subcutaneous injection. Namilumab is a potent GM-CSF inhibitor that has been well-tolerated so far in more than 350 participants across multiple clinical trials. Evidence from non-clinical studies indicate that GM-CSF promotes macrophage and dendritic cell activity which contributes to granuloma formation. Inhibiting GM-CSF can reduce the presence of granulomas and the resulting inflammation, potentially leading to a reduction in symptoms and resolution of the underlying disease. About Kinevant Sciences Kinevant Sciences, a subsidiary of Roivant, is a clinical-stage biopharmaceutical company developing new medicines for rare autoimmune and inflammatory diseases. The company takes a patient-first approach to drug development, advancing candidates with the potential to resolve the underlying disease and create life-changing benefit for patients. Kinevant is initially focused on the development of namilumab for the treatment of sarcoidosis, a multi-organ systemic disease with a high unmet medical need. For more information, visit or follow us on LinkedIn. About Roivant Roivant is a commercial-stage biopharmaceutical company that aims to improve the lives of patients by accelerating the development and commercialization of medicines that matter. Today, Roivant’s pipeline includes VTAMA®, a novel topical approved for the treatment of psoriasis and in development for the treatment of atopic dermatitis; batoclimab and IMVT-1402, fully human monoclonal antibodies targeting the neonatal Fc receptor (“FcRn”) in development across several IgG-mediated autoimmune indications; brepocitinib, a novel TYK2/JAK1 inhibitor in late stage development for dermatomyositis, non-infectious uveitis, and other autoimmune conditions, in addition to other clinical stage molecules. We advance our pipeline by creating nimble subsidiaries or “Vants” to develop and commercialize our medicines and technologies. Beyond therapeutics, Roivant also incubates discovery-stage companies and health technology startups complementary to its biopharmaceutical business. For more information, .

Phase 2Clinical ResultDrug Approval

02 Apr 2024

·www.fiercebiotech.com

Roivant's inflammatory med gets back on track with phase 2 eye disease data

Roivant expects to launch brepocitinib into a phase 3 NIU trial by the second half of the year. Roivant’s autoimmune treatment impressed in a phase 2 trial, reporting treatment failure rates among patients with non-infectious uveitis (NIU) that executives touted as the best seen in active studies. The company, known for turning shelved pharma assets into valued medicines, believes it has struck gold once more, with Roivant's leadership using Tuesday’s readout to allude to brepocitinib’s blockbuster potential. “With data like the data we're generating, we just feel highly confident,” CEO Matt Gline told investors. The phase 2 trial enrolled 26 patients with the inflammatory eye condition, with 17 receiving 45 mg of brepocitinib and nine receiving a 15 mg dose. Roivant found that at week 24, 29% of patients receiving 45 mg of once-daily brepocitinib and 44% of patients receiving 15 mg reached the pre-specified criteria for treatment failure, meeting the study's primary endpoint. Treatment failure was defined as a worsening in one of three measurements assessing either vision or eye irritation, where lower rates are indicative of greater benefits from the therapy. When discontinuations were censored from the analysis, the treatment failure rate for the 45 mg arm was 18%. The treatment failure rates at both doses were lower than the performance of AbbVie's blockbuster Humira in a previous phase 3 trial for NIU, the company pointed out in a presentation to investors. Roivant also reported that all secondary endpoints were “positive and dose-responsive” at the 24-week mark. “Against that backdrop, we are thrilled to see a failure rate of only 29% in the brepocitinib 45 mg arm, better than any precedent study was able to achieve even with more lenient tapers,” Ben Zimmer, CEO of Roivant's Priovant unit, said in a release. Roivant said brepocitinib was well-tolerated with one treatment-emergent adverse event reported in the 15 mg dose group. No new safety signals have arisen, the company added. Brepocitinib was snagged from Pfizer in 2022. Roivant had also been exploring the drug in lupus but dropped that program in November after it failed to demonstrate an improvement in disease activity in a phase 2 study. Luckily for Roivant, today's readout means it’s full-steam ahead for brepocitinib development in NIU, including a phase 3 trial slated to get underway in the second half of 2024. Gline said it’s “relatively unlikely” that Roivant would include a Humira comparator arm in the upcoming late-stage study but said plans will be cemented after an end-of-phase-2 meeting with the FDA. As for the asset’s dermatomyositis indication, a phase 3 trial is set to be fully enrolled by the third quarter. On today's call, Zimmer loosely co-signed an investor’s back-of-the-napkin math that data could be expected in the second half of 2025. The expectation is that more indications could soon be tacked onto the development plan, with Gline telling investors: “We have a lot of ideas.” “Every time we read out positive data with this compound and look at it, it makes us feel like we should be doing more with it,” Gline added.

Phase 2Phase 3Clinical ResultClinical Trial Failure

100 Deals associated with Brepocitinib

External Link

KEGG	Wiki	ATC	Drug Bank
D11537	-	-	DB15003

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Uveitis, Intermediate	Phase 3	-	Priovant Therapeutics, Inc.	23 Aug 2024
Uveitis, Posterior	Phase 3	-	Priovant Therapeutics, Inc.	23 Aug 2024
Dermatomyositis	Phase 3	US	Priovant Therapeutics, Inc.	28 Jun 2022
Colitis, Ulcerative	Phase 2	DK	Pfizer Inc.	03 Feb 2017
Alopecia Areata	Phase 2	AU	Pfizer Inc.	15 Dec 2016
Alopecia Areata	Phase 2	US	Pfizer Inc.	15 Dec 2016
Plaque psoriasis	Phase 2	CA	Pfizer Inc.	01 Dec 2016
Plaque psoriasis	Phase 2	PL	Pfizer Inc.	01 Dec 2016
Plaque psoriasis	Phase 2	US	Pfizer Inc.	01 Dec 2016
Alopecia Areata	Discovery	CA	Pfizer Inc.	15 Dec 2016

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05523765 (NEPTUNE, Biospace) Manual	Phase 2	Uveitis	26	brepocitinib 45 mg	(hooeipuzfw) = unbxrzujoe shprbrykla (zyrftwsyip ) Met View more	Positive	02 Apr 2024
NCT04260464 (CTgov)	Phase 1	Renal Insufficiency	30	PF-06700841 (Severe Renal Impairment)	(pzaqibwmma) = hkceydshfp tpaakonzru (lvqxnqgtgc, gksfojnqni - zfuhnjsuwc) View more	-	22 Jan 2024
				PF-06700841 (Normal Renal Function)	(pzaqibwmma) = rsgjgfaasn tpaakonzru (lvqxnqgtgc, zxaqbcorsk - wosikwkzoz) View more
GlobeNewswire Manual	Phase 2	Systemic Lupus Erythematosus	-	Brepocitinib	(lmppsxwexg) = Oral brepocitinib failed to meet its primary endpoint of Systemic Lupus Erythematosus Responder Index (SRI-4) change of 4 at Week 52 drrpmdwvsv (sjleogdhqz ) Not Met View more	Negative	27 Nov 2023
NCT04092452 (CTgov)	Phase 2	Hidradenitis Suppurativa	194	placebo+PF-06826647+PF-06700841+PF-06650833 (Placebo)	whrazavcbn(slwfdymzbr) = kleflbvwqw ptqysdongo (fosoyiiuqk, pbshndzdmt - hgdrcwczfm) View more	-	15 Jun 2023
				PF-06650833 (PF-06650833 400mg QD)	whrazavcbn(slwfdymzbr) = amzrtaeuob ptqysdongo (fosoyiiuqk, rovmvhepnt - umjtarceni) View more
Pubmed	Not Applicable	Arthritis, Psoriatic	218	Brepocitinib 30 mg QD	(twfhuvrofs) = plknxuzxpq rjdwnxgojx (hdnzaeruwf )	Positive	17 May 2023
				Brepocitinib 60 mg QD	(twfhuvrofs) = sroypdfwnz rjdwnxgojx (hdnzaeruwf )
NCT03770039 (Pubmed)	Phase 1	-	6	Brepocitinib	etzabboyna(kpdjddrdfg) = Brepocitinib was absorbed rapidly following oral administration ebrvvunwto (fnihuphdro )	-	15 May 2023
NCT02958865 (Pubmed)	Phase 2	Colitis, Ulcerative	319	Ritlecitinib 20 mg	ejgixoevit(tdyoulngez) = One death due to myocardial infarction (ritlecitinib) allsrsvnkm (igdchjiuss ) View more	Positive	06 Jan 2023
				Ritlecitinib 70 mg
NCT02974868 (ALLEGRO, Pubmed) Manual	Phase 2	Alopecia Areata	23	brepocitinib	ieauxdvxes(lmttotcbyj) = An exploratory efficacy evaluation showed that none of the five patients receiving ritlecitinib in the crossover open-label extension achieved ≥30% improvement from baseline in Severity of Alopecia Tool score or improvement in eyebrow/eyelash assessments. dpvrdoykqy (mbtfbsyrrw )	Positive	07 Sep 2022
				Ritlecitinib
NCT03963401 (CTgov)	Phase 2	Arthritis, Psoriatic	219	Placebo+PF-06700841 (Placebo)	fxhxnbduow(erdyuzdwem) = otlpyxpvml foqbkvcznk (uocyalgwwe, qrmjbugmbi - cflqvgxemf) View more	-	04 Aug 2021
				PF-06700841 (PF-06700841 10 mg QD)	fxhxnbduow(erdyuzdwem) = skdwlckzpz foqbkvcznk (uocyalgwwe, keeegwvril - hqarbujxoz) View more
NCT02969018 (Pubmed) Manual	Phase 2	Plaque psoriasis	212	PF-06700841	(proeluazyv) = buwdbfqgsc xadmhhbjvg (pbardepyjk, -20.0 ~ -14.6) View more	Positive	01 Dec 2020
				Placebo	-

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Leverages most recent intelligence information, enabling fullest potential.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis