An Open-label, Single-arm Study to Evaluate Pharmacokinetics, Pharmacodynamic Effects, Safety and Tolerability of Fenebrutinib in Children and Adolescents With Relapsing Multiple Sclerosis

This open label, single arm study will evaluate the PK and PD effects of fenebrutinib in children and adolescents with RMS aged between 10 and < 18 years.
This study consists of a Dose Exploration Period and an Optional Extension Period. Eligible participants may choose to continue treatment with fenebrutinib in the optional extension period after completing the dose exploration period.

Start Date06 Oct 2025

Sponsor / Collaborator

Hoffmann-La Roche Ltd.

ISRCTN41455091

/ RecruitingPhase 1

A phase I, open-label, single-dose study to evaluate the effect of severe renal impairment on the pharmacokinetics of fenebrutinib

Start Date06 Jun 2024

Sponsor / Collaborator

Genentech, Inc.

ISRCTN46432183

/ RecruitingPhase 1

A phase I, open-Label, single-Dose study to evaluate the effect of mild or moderate hepatic impairment on the pharmacokinetics of fenebrutinib

Start Date18 Oct 2023

Sponsor / Collaborator

Genentech, Inc.

100 Clinical Results associated with Fenebrutinib

100 Translational Medicine associated with Fenebrutinib

100 Patents (Medical) associated with Fenebrutinib

Literatures (Medical) associated with Fenebrutinib

02 Sep 2025·NATURAL PRODUCT RESEARCH

Molecular docking based comparative study of antiviral compounds on SARS-CoV-2 spike protein

Article

Author: Biswal, Pradyut K. ; Kumar, Jitendra ; Nagavarapu, Sowmya

The urgent need for effective therapeutic interventions against SARS-CoV-2 has prompted extensive exploration of potential drug candidates. Among the viral proteins, the spike (S) protein presents an attractive target due to its critical role in viral entry and infection. In this study, we employed molecular docking techniques to investigate the binding affinities and interaction profiles of a panel of active compounds against the SARS-CoV-2 spike protein. Utilising computational simulations, we assessed the binding properties of these compounds within the receptor-binding domain (RBD) and other key regions of the spike protein. Our comparative analysis elucidates the differential binding patterns and identifies promising lead compounds with high binding affinity and favourable interaction profiles. Furthermore, we discuss the implications of these findings for the development of potential therapeutics targeting the SARS-CoV-2 spike protein. Using molecular docking and the Lipinski five rule, this study illustrates possible compounds with strong binding affinities, their molecular interactions, for both naturally occurring and man-made drugs. Computational approach is applied, and it is concluded that, drugs like Withanolide, Dihydroergocristine, Fenebrutinib, and Ergotamine shows binding energies between -8.3 and -9.1 kcal/mol, and are possible candidate for anti covid drug.

01 Sep 2025·EUROPEAN JOURNAL OF PHARMACOLOGY

Next generation Bruton's tyrosine kinase inhibitors – characterization of in vitro potency and selectivity

Article

Author: Angst, Daniela ; Cenni, Bruno ; Pulz, Robert

Bruton's tyrosine kinase (BTK) mediates B cell receptor and Fc receptor signaling and is a key regulator of autoimmunity and allergy. A series of novel BTK inhibitors (BTKi) are currently in development for non-oncologic indications with covalent-irreversible (remibrutinib, evobrutinib, tolebrutinib, orelabrutinib), covalent-reversible (rilzabrutinib), and non-covalent reversible (fenebrutinib) binding modes. This study characterizes their in vitro potency and selectivity profiles under the same conditions to minimize assay differences across the different binding modes. Covalent BTKi showed human in vitro blood BTK binding in a time- and concentration-dependent manner with remibrutinib being the most potent and fastest in onset of action. Cellular BTK pathway inhibition was determined in human blood B cells and basophils, and for covalent BTKi correlated well with BTK binding. In contrast to the covalent-irreversible remibrutinib, the non-covalent reversible fenebrutinib showed rapid loss of cellular BTK inhibition after washout. Kinase selectivity was assessed in a binding screen across the human kinome, followed by quantification of binding affinities for a selection of kinases. BTKi ranked in their selectivity as follows (most selective to least): remibrutinib, fenebrutinib, evobrutinib, orelabrutinib, rilzabrutinib and tolebrutinib. These data suggest that next generation BTKi show important differences in their in vitro target binding and selectivity when compared under the same conditions.

01 Aug 2025·LANCET NEUROLOGY

Safety and efficacy of fenebrutinib in relapsing multiple sclerosis (FENopta): a multicentre, double-blind, randomised, placebo-controlled, phase 2 trial and open-label extension study

Article

Author: Habek, Mario ; Kuruvilla, Denison ; Qi, Qi ; Hua, Le H ; Budincevic, Hrvoje ; Xu, Yan ; Goodyear, Alexandra ; Dufek, Michal ; Drulovic, Jelena ; Mitzner, Maresa Caunt ; Bar-Or, Amit ; Ratchford, John N ; Weber, Martin S ; Napieralski, Julie ; Thomas, Piia ; Harp, Christopher T ; Chen, Ying-Fang ; Clayton, David ; Oh, Jiwon

BACKGROUND:

The prospect for Bruton's tyrosine kinase (BTK) inhibition to meaningfully affect relapsing multiple sclerosis has recently been questioned due to inconsistent findings in the magnitude and sustainability of the effect of BTK inhibitors on disease activity. We assessed the safety, efficacy, and CSF drug concentrations of fenebrutinib, a highly selective, noncovalent, reversible BTK inhibitor, in patients with relapsing multiple sclerosis.

METHODS:

This multicentre, double-blind, randomised, placebo-controlled, phase 2 trial (FENopta) was conducted at 18 community centres and hospitals across six countries in Europe and North America. Patients with relapsing multiple sclerosis aged 18-55 years with an Expanded Disability Status Scale (EDSS) score of 0·0-5·5, and recent documented disease activity, were randomly assigned (2:1) to oral fenebrutinib (200 mg twice daily) or placebo for 12 weeks, using permuted blocks and stratified by the presence or absence of T1 gadolinium-enhancing (Gd+) lesions on the brain MRI at screening. The randomisation sequence was generated by an interactive voice or web response system and both patients and investigators were masked to treatment allocation. Participants could enter an optional open-label extension study to receive fenebrutinib for up to 192 weeks. The primary efficacy endpoint was the total number of new T1 Gd+ lesions on brain MRI at weeks 4, 8, and 12; with additional MRI assessments at 48-week intervals during the open-label extension. Efficacy analyses were done on randomised patients with evaluable post-baseline MRIs; safety analyses used the safety-evaluable population. This study is registered with ClinicalTrials.gov, NCT05119569, and EudraCT, 2021-003772-14; recruitment is closed and the trial is ongoing.

FINDINGS:

Between March 1, 2022 and March 29, 2023, 109 patients with relapsing multiple sclerosis were randomly assigned treatment: 73 received fenebrutinib and 36 received placebo. 106 patients had evaluable post-baseline brain MRI scans and were assessed for efficacy in the fenebrutinib group (n=70) and placebo group (n=36). The combined number of new T1 Gd+ lesions at weeks 4, 8, and 12 were 0·077 (95% CI 0·043-0·135) in the fenebrutinib group and 0·245 (0·144-0·418) in the placebo group (69% relative reduction [95% CI 34-85]; p=0·0022). During the open-label extension, through week 48, the unadjusted annualised relapse rate was 0·04 and 95 (96%) of 99 patients were relapse-free. During the double-blind treatment phase, the most common adverse events that were more frequent in the fenebrutinib group than in the placebo group were hepatic enzyme elevations (four [6%] vs 0), headache (three [4%] vs one [3%]), and nasopharyngitis (two [3%] vs 0); no serious adverse events or deaths occurred.

INTERPRETATION:

Fenebrutinib was well tolerated and exerted an early, robust, and sustained effect of limiting new focal brain lesions. Further studies are needed to better characterise the safety and efficacy of fenebrutinib on both relapsing multiple sclerosis and non-relapsing progressive multiple sclerosis.

FUNDING:

F. Hoffmann-La Roche.

News (Medical) associated with Fenebrutinib

15 Nov 2025

·endpoints.news

Inside the Metsera bidding war; PD-(L)1xVEGF bispecific race heats up; Pazdur tapped as next CDER head; and more

Welcome back to Endpoints Weekly. It’s going to be a chilly weekend here in Boston, with low temperatures dipping into the 30s — the perfect weather for a warm cup of tea while recapping another busy week in biopharma. If you haven’t already, be sure to read the Endpoints team’s exclusive on how Pfizer closed its deal with Metsera. We also have a feature from Max Gelman on how competition is stacking up in the PD-(L)1xVEGF space, details on Richard Pazdur’s appointment to CDER, some positive results for Roche’s BTK inhibitor, and the story behind a new VC firm hunting for the next big advances in obesity treatment. We’ll be back on Monday. Until then, stay warm! — Nicole DeFeudis 💇‍♂️Pfizer completed its up to $10 billion acquisition of the obesity biotech Metsera this week, ending a high-stakes bidding war between Pfizer and Novo Nordisk. Last week, we reported that Metsera had accepted Pfizer’s offer after the FTC warned the biotech that Novo’s bid was risky under US antitrust law. But you can see exactly how the final deal unfolded in this exclusive by Endpoints’ Elizabeth Cairns, Kyle LaHucik and Drew Armstrong — including how Metsera’s co-founder Paul Berns was in the middle of a haircut when he was alerted that Novo was submitting its surprise offer. The deal gives Pfizer a fresh chance in obesity after the company dropped its obesity pill danuglipron in April. Novo fought hard for Metsera, as it looks to maintain a leading stake in the obesity market. But even though Pfizer won the battle, all eyes will be on how the experimental drugs it acquired perform in trials. Stay tuned. 🏎️ Drugmakers in the PD-(L)1xVEGF space are revving their engines, Endpoints’ Max Gelman reported this week. While much of the focus has been on Summit Therapeutics and its lead drug ivonescimab, two other rival teams have recently detailed their clinical development plans. Check out Max’s in-depth look at the competition here. One of the challengers is Pfizer and 3SBio, which inked a licensing deal for a PD-1xVEGF bispecific called SSGJ-707, or PF’4404, earlier this year. Pfizer said on Monday that among other trials, it has plans for a Phase 3 study in first-line metastatic colorectal cancer and a Phase 3 non-small cell lung cancer study evaluating both squamous and non-squamous tumors. Bristol Myers Squibb and BioNTech are also in the running. They teamed up this year to advance a PD-L1xVEGF program that BioNTech got in its Biotheus acquisition. Bristol Myers outlined plans for five mid- and late-stage studies during an earnings call last month, and BioNTech said this week that it’s also looking at studies in pancreatic cancer, ovarian cancer and glioblastoma. Both companies intend to look at combinations within their respective pipelines, Max reported. Despite all the momentum, the race could take a while to play out as Summit plans to launch more studies and we wait for key data from Pfizer and BMS. Longtime cancer chief Richard Pazdur was appointed to lead the Center for Drug Evaluation and Research, just over a week after former director George Tidmarsh’s sudden resignation. Pazdur has 26 years of experience at the agency and is the founding director of the FDA’s Oncology Center of Excellence. During his time at the FDA, he has been focused on speeding up the development of new cancer therapies. Pazdur vs. Prasad: Current CBER Director Vinay Prasad previously criticized Pazdur in social media posts before Prasad joined the FDA. Endpoints’ Zachary Brennan analyzed the complex dynamic and the events that led to Pazdur’s appointment here. 💵Two former executives of Lilly’s diabetes unit have launched a venture capital firm called 501 Ventures, and they’re looking for the next approaches to obesity treatment. The firm will fund science for next-generation metabolic health medicines. Its founders, Enrique Conterno and Meg Powell, wouldn’t disclose the amount of capital they’re working with so far. But Powell said they’ll court pharma companies to help support the fund. Kyle LaHucik reported the details from this year’s ObesityWeek conference in Atlanta. Read more here . Roche reported positive results from two separate Phase 3 trials that tested fenebrutinib in relapsing multiple sclerosis and primary progressive multiple sclerosis. Roche hasn’t shared the detailed results, but CMO Levi Garraway described the wins as “unprecedented.” Roche said it will wait for data from a second Phase 3 RMS trial before finalizing regulatory filing plans.

Phase 3Executive ChangeAcquisitionLicense out/in

11 Nov 2025

·pmlive.com

Genentech announces positive clinical results for BTK inhibitor MS treatment

Genentech, a member of the Roche Group, has announced positive results from the first of two phase 3 trials investigating fenebrutinib, the first and only Bruton’s tyrosine kinase (BTK) inhibitor in development for the treatment of relapsing multiple sclerosis (RMS). Multiple sclerosis (MS) is a chronic neurological condition affecting more than 2.9 million people globally. Approximately 85% of patients are diagnosed with RMS, which is characterised by relapses and progressive disability over time. The remaining 15% have primary progressive multiple sclerosis (PPMS), a form marked by continuous worsening of symptoms without relapses or remissions. Currently, the only treatment approved by the US Food and Drug Administration (FDA) for PPMS is Ocrevus (ocrelizumab). Fenebrutinib is an investigational, oral BTK inhibitor that targets both B cells and microglia in the immune system. This dual mechanism of action is designed to address key drivers of MS pathology: B-cell inhibition helps to control the acute inflammation responsible for relapses, while targeting microglia within the central nervous system may limit chronic damage and slow long-term disability progression. According to Genentech, fenebrutinib’s high potency, selectivity and reversibility are driven by its non-covalent binding properties, distinguishing it from other treatments currently in development. Results from the randomised, double-blind, double-dummy, parallel-group FENhance 2 study showed that fenebrutinib met its primary endpoint, significantly reducing the annualised relapse rate (ARR) in patients with RMS compared with teriflunomide over 96 weeks of treatment. Results from FENhance 1, the second phase 3 trial in the RMS programme, are expected in the first half of 2026. In addition, the phase 3 FENtrepid study, which evaluated fenebrutinib versus Ocrevus in patients with PPMS, also met its primary endpoint. Fenebrutinib demonstrated non-inferiority to Ocrevus in delaying the onset of composite confirmed disability progression over the treatment period. “Fenebrutinib substantially reduced the number of relapses in RMS and slowed disability progression in PPMS. These unprecedented results suggest that fenebrutinib could potentially become a best-in-disease medicine as the first high-efficacy, oral treatment for people with RMS or PPMS,” said Levi Garraway, Genentech’s chief medical officer and head of Global Product Development. “Therefore, these pivotal results for fenebrutinib may offer new hope for people living with MS, and they reaffirm our enduring commitment to the MS community.”

Clinical ResultPhase 3Drug ApprovalPhase 2

10 Nov 2025

·pharma.economictimes.indiatimes.com

Roche's experimental MS drug hits main goal in one of two key trials

Frankfurt: Roche 's experimental multiple sclerosis drug achieved its main goal in one of two key late-stage trials testing it against the relapsing form of the disease, the Swiss drugmaker said on Monday, sending its shares up nearly 2%. The drug, fenebrutinib , was shown to significantly reduce the annualised relapse rate when compared with another drug teriflunomide , over a period of at least 96 weeks of treatment, the company said in a statement. Teriflunomide is sold under the brand name Aubagio by French drugmaker Sanofi. If successful, the drug could provide MS patients a new treatment option and bring in over $1 billion in annual peak sales for Roche , according to Leerink analysts. In a separate third study, Roche's drug candidate was shown to be at least as effective as its own Ocrevus drug in delaying the progression of another form of the disease known as primary progressive multiple sclerosis , the company said. SECOND LATE-STAGE STUDY DATA DUE IN FIRST HALF OF 2026 Roche said data from the second late-stage study against relapsing MS is expected by the first half of 2026. In late 2023, the U.S. FDA had stopped enrollment of new patients in this study, citing cases of liver injury. Roche said on Monday that liver safety was consistent with previous trials. It plans to share detailed data from both the studies at an upcoming medical meeting and will submit data from all three studies to regulatory authorities. Jefferies analysts said that the success of Roche's regulatory submissions for the drug are critically dependant on full safety and efficacy data from the three studies. Fenebrutinib belongs to a class of compounds known as Bruton's tyrosine kinase (BTK) inhibitors, where Sanofi is also a contestant in a development race that has seen trial setbacks by other drugmakers. The class of drugs is designed to selectively block the harmful autoimmune reaction behind MS for a more targeted approach than standard immunosuppressant therapy. (Reporting by Ludwig Burger and Bhanvi Satija in London; Editing by Christian Schmollinger, Jamie Freed and Conor Humphries)

100 Deals associated with Fenebrutinib

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Multiple sclerosis relapse	Phase 3	United States	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	China	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Argentina	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Dominican Republic	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Finland	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Germany	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Hong Kong	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Hungary	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Italy	Hoffmann-La Roche, Inc.	17 Mar 2021
Multiple sclerosis relapse	Phase 3	Kenya	Hoffmann-La Roche, Inc.	17 Mar 2021

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05119569 (FENopta, Company_Website) Manual	Phase 2	Multiple sclerosis relapse	99	fenebrutinib	leliqrprku(qvpwfrthsv) = myoledbkes rgkgmvuajy (sobunhtmge )	Positive	30 May 2025
NCT05119569 (FENopta, AAN2025)	Phase 2	Multiple sclerosis relapse	99	Fenebrutinib 200 mg	zwrmfjqkon(acaoklwcvq) = An asymptomatic alanine transaminase elevation occurred newly in one OLE participant (1%) that resolved feyqbdzvqn (wuhygzozdf ) View more	Positive	07 Apr 2025
				Placebo
NCT05119569 (FENopta-OLE, GlobeNewswire) Manual	Phase 2	Multiple sclerosis relapse	109	Fenebrutinib	grhpslkfpu(cjfpmxdmfe) = xpxzrivthi dwkftbdhqc (oupxpoheqx ) View more	Positive	04 Sep 2024
AAN2024	Phase 1	-	-	Fenebrutinib 400 mg	mwzggovokb(afepadiaon) = Both doses were well tolerated, and no serious adverse events (AEs), AEs of special interest or Grade ≥2 AEs were reported altynvilar (ubkmkduoma )	Positive	09 Apr 2024
				Fenebrutinib 700 mg
NCT04586010 (FENhance, Biospace) Manual	Phase 3	Multiple sclerosis relapse	-	fenebrutinib	ehpuudqdgc(cdycgzpuxp) = zucvfxogkm goxzzqgwrk (xenkyowhlv )	Negative	05 Dec 2023
NCT05119569 (FENopta, ECTRIMS2023) Manual	Phase 2	Multiple Sclerosis	106	Fenebrutinib 200 mg	vbozcqfsjw(eqnrtxwlvn) = gscmbplfyc aysohkzthk (tnyijjwbfj ) View more	Positive	17 Oct 2023
				Placebo	vbozcqfsjw(eqnrtxwlvn) = ddtjxqjlhw aysohkzthk (tnyijjwbfj ) View more
Fenebrutinib (EULAR2021)	Phase 2	Systemic Lupus Erythematosus C3 \| C4 \| ANA ... View more	260	Fenebrutinib	bzrkfavurb(ltmfzmlbzn) = foepajfejj ylaylppfru (vlkfvklorc )	-	02 Jun 2021
NCT03407482 (CTgov)	Phase 2	Systemic Lupus Erythematosus	160	GDC-0853	anounsfkms = azirjyhhir xqtmesbqkq (oftlpvxdyk, muwwtaersd - apqxvtsmfv) View more	-	19 Dec 2020
NCT03137069 (CTgov)	Phase 2	Chronic Urticaria	134	Placebo (Cohort 1: Placebo)	vfgpepvfzo(galmtcfpez) = pbpbcyhahl fdnpfzigaq (tcqodoyeab, 13.49) View more	-	29 Sep 2020
				GDC-0853 (Cohort 1: GDC-0853 200mg BID)	vfgpepvfzo(galmtcfpez) = zoppkjwicf fdnpfzigaq (tcqodoyeab, 9.74) View more
NCT03693625 (CTgov)	Phase 2	Chronic Urticaria	31	GDC-0853 (Parent Study: GDC-0853)	etripstspp = srxxvpxsnc wtfrselwbh (kxxcpcndhf, wflckgntly - ahuqwdxrid) View more	-	25 Sep 2020
				GDC-0853 (Parent Study: Placebo)	etripstspp = uhqqihbchy wtfrselwbh (kxxcpcndhf, fjqdrlfodo - jnxkerdnxv) View more

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