NTRK inhibitors(Neurotrophic tyrosine kinase receptor inhibitors), ROS1 inhibitors(Proto-oncogene tyrosine-protein kinase ROS inhibitors), TrkA antagonists(Nerve growth factor receptor Trk-A antagonists)

Therapeutic Areas

NeoplasmsRespiratory Diseases

Active Indication

Reactive oxygen species 1 positive non-small cell lung cancerAdvanced Lung Non-Small Cell Carcinomametastatic non-small cell lung cancer

Inactive Indication

Advanced Malignant Solid NeoplasmCDH1 Mutation Invasive Lobular Breast CarcinomaMetastatic breast cancer+ [1]

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Nuvation Bio, Inc.

AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup

Asymchem Life Science Tianjin Co. Ltd.

+ [1]

Inactive Organization

Daiichi Sankyo Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

CN (17 Dec 2024),

Reactive oxygen species 1 positive non-small cell lung cancer

RegulationPriority Review (US), Breakthrough Therapy (US), Orphan Drug (US), Priority Review (CN), Breakthrough Therapy (CN), Conditional marketing approval (CN)

Structure

Molecular FormulaC23H24FN5O

InChIKeyHEVHTYMYEMEBPX-HZPDHXFCSA-N

CAS Registry1505514-27-1

Clinical Trials associated with Taletrectinib

NCT06214793 / SuspendedPhase 2IIT

A Phase II Study of Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC) of the Breast (TaCe)

The purpose of this study is to evaluate the safety and tolerability of talectrectinib as treatment for Stage IV ILC with CDH1 mutation

Start Date01 Apr 2025

Sponsor / Collaborator

The Case Comprehensive Cancer Center

[+1]

NCT06564324 / Not yet recruitingPhase 3

A Phase 3 Multicenter Open-label Study of Taletrectinib Versus a Standard of Care ROS1-Tyrosine Kinase Inhibitor (Crizotinib) in TKI-Naïve Patients With ROS1-Positive Locally Advanced or Metastatic Non-Small Cell Lung Cancer (TRUST-III)

This is a Phase 3, randomized, open-label, comparative, multicenter, international study for NSCLC patients whose tumor tissue exhibits ROS1 fusion positivity (i.e., ROS1+) and who have not previously received an ROS1-targeted TKI (i.e., ROS1-TKI-naïve).
Approximately 138 ROS-1 TKI- naïve ROS1+NSCLC patients will be randomized in a 1:1 ration to one of 2 study arms:
* Arm A: Taletrectinib monotherapy at 600 mg once daily (QD), continuously;
* Arm B: Crizotinib monotherapy at 250 mg twice daily (BID), continuously. Each cycle duration will be 28 days.
Participants will be stratified by the presence of intracranial metastases at baseline (Yes versus No) and prior chemotherapy use for locally advanced or metastatic disease (Yes versus No). For the purposes of stratification, prior chemotherapy is defined as completion of ≥1 cycle of chemotherapy in the locally advanced or metastatic setting. Participants will be treated until they experience progressive disease (PD) assessed by the BIRC, intolerable toxicity, or another discontinuation criterion is met. Crossover from control group (crizotinib) to taletrectinib is also permitted, at the Investigator's discretion with the Sponsor's approval, for qualifying participants who have experienced objective progression confirmed by the BIRC.

Start Date01 Sep 2024

Sponsor / Collaborator

AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup

NCT05609929 / CompletedPhase 1

A Phase I, Single-center, Open-label, Fixed Sequence Study in Chinese Healthy Male Adults to Evaluate the Effect of Omeprazole on the Pharmacokinetics of AB-106

This is a single-center, open-label, fixed sequence phase I clinical study. To evaluate the effect of continuous administration of omeprazole magnesium enteric coated tablets on PK after single dose AB-106 capsule administration in Chinese healthy male subjects. This study includes a screening period (1-28 days before administration), treatment period (34 days), and follow-up period ( after the last dose completed 7 ± 3 days). The treatment period of this study was divided into two periods, and the subjects were divided into two groups, 12 subjects in the first group and 10 subjects in the second group. The treatment method and research process of each group of subjects are the same. After the first group of subjects completes the second cycle and is evaluated by the investigator and sponsor, the second group of subjects can start administration. If there are no more than 4 subjects in the first group who have vomiting gastrointestinal reaction (vomiting occurs within 8 hours after each cycle of administration) after completing the two cycles of administration of AB-106 400 mg, they can be added to the second group of subjects, and the number of added subjects shall not exceed the number of subjects who have vomiting gastrointestinal reaction. If more than 4 subjects have gastrointestinal reaction of vomiting, the investigator and sponsor will make a comprehensive evaluation, and can reduce the dosage of AB-106 to 200 mg, and 22 subjects will be included in the trial at one time or supplemented in the second group to complete the 400 mg dose group

Start Date02 Nov 2022

Sponsor / Collaborator

Nuvation Bio, Inc.

[+1]

100 Clinical Results associated with Taletrectinib

100 Translational Medicine associated with Taletrectinib

100 Patents (Medical) associated with Taletrectinib

Literatures (Medical) associated with Taletrectinib

01 Oct 2024·JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES

Application of newly developed and validated UPLC-MS/MS method for pharmacokinetic study of ROS1/NTRK inhibitor taletrectinib in beagle dog plasma

Article

Author: Zhu, Yunfeng ; Fan, Ali ; Wang, Xin ; Wang, Fangkai ; Cheng, Ya ; Wang, Xingyu ; Chang, Jiawei

Taletrectinib is a potent selective ROS and pan-NTRK tyrosine kinase inhibitor (TKI) and has been developed to treat non-small cell lung cancer (NSCLC). To facilitate pharmacokinetic and toxicokinetic studies of taletrectinib, we developed a procedure for ultra-high-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) to detect the plasma level of taletrectinib in dogs. This assay procedure was validated in compliance with FDA guidance. The dog plasma samples were spiked with internal standard (IS), followed by protein precipitation, and analyzed using a Waters ACQUITY BEH C₁₈ column coupled to a Thermo triple quadrupole mass spectrometer. Separation was executed using the acetonitrile-0.1 % formic acid solution with gradient elution, at a flow rate of 0.4 mL/min. Taletrectinib and IS were monitored by multiple reaction monitoring (MRM) with m/z 406.2 > 349.2 and m/z 441.2 > 138.1, respectively. The procedure demonstrated excellent linearity with a correlation coefficient greater than 0.999 within the concentration range of 0.2-200 ng/mL. The inter- and intra-day accuracy ranged from -5.25 % to 5.26 %, and the precision was below 6.39 %. Acetonitrile-mediated protein precipitation showed high extraction efficiency and a recovery above 85 %. The procedure was then applied to quantify taletrectinib in beagle dog plasma after oral and intravenous doses and achieved success. The obtained pharmacokinetic parameters indicated high bioavailability of taletrectinib (>85 %) and extensive tissue distribution (>40 L/kg).

01 Sep 2024·BIOORGANIC CHEMISTRY

Discovery of a first-in-class protein degrader for the c-ros oncogene 1 (ROS1)

Article

Author: Ou, Hongyue ; Liu, Haixia ; Yang, Jiawen ; Qu, Xiaojuan ; Song, Xiaoling ; Zhu, Qiaoliang ; Wei, Yongqi ; Ge, Di ; Lu, Chunlai ; Wu, Yifan ; Jiang, Biao

The c-ros oncogene 1 (ROS1), an oncogenic driver, is known to induce non-small cell lung cancer (NSCLC) when overactivated, particularly through the formation of fusion proteins. Traditional targeted therapies focus on inhibiting ROS1 activity with ROS 1 inhibitors to manage cancer progression. However, a new strategy involving the design of protein degraders offers a more potent approach by completely degrading ROS1 fusion oncoproteins, thereby effectively blocking their kinase activity and enhancing anti-tumour potential. Utilizing PROteolysis-TArgeting Chimera (PROTAC) technology and informed by molecular docking and rational design, we report the first ROS1-specific PROTAC, SIAIS039. This degrader effectively targets multiple ROS1 fusion oncoproteins (CD74-ROS1, SDC4-ROS1 and SLC34A2-ROS1) in engineered Ba/F3 cells and HCC78 cells, demonstrating anti-tumour effects against ROS1 fusion-driven cancer cells. It suppresses cell proliferation, induces cell cycle arrest, and apoptosis, and inhibits clonogenicity. The anti-tumour efficacy of SIAIS039 surpasses two approved drugs, crizotinib and entrectinib, and matches that of the top inhibitors, including lorlatinib and taletrectinib. Mechanistic studies confirm that the degradation induced by 039 requires the participation of ROS1 ligands and E3 ubiquitin ligases, and involves the proteasome and ubiquitination. In addition, 039 exhibited excellent oral bioavailability in a mouse xenograft model, highlighting its potential for clinical application. In conclusion, our study presents a promising and novel therapeutic strategy for ROS1 fusion-positive NSCLC by targeting ROS1 fusion oncoproteins for degradation, laying the foundation for the development of further PROTAC and offering hope for patients with ROS1 fusion-positive NSCLC.

01 Aug 2024·JOURNAL OF CLINICAL ONCOLOGY

Efficacy and Safety of Taletrectinib in Chinese Patients With ROS1+ Non–Small Cell Lung Cancer: The Phase II TRUST-I Study

Article

Author: Lu, Kaihua ; Wu, Jingxun ; Wang, Yongsheng ; Qin, Xintian ; Yang, Nong ; Zhuang, Wu ; Wang, Ziping ; Zhang, Xianyu ; Meng, Xue ; Li, Wei ; Wang, Xicheng ; Fan, Huijie ; Lovly, Christine M. ; Yan, Bing ; Liu, Yunpeng ; Ren, Yizhong ; Zhao, Yanqiu ; Zhou, Caicun ; Xiong, Anwen ; Yu, Qitao

PURPOSE:

Taletrectinib, a highly potent, CNS-active, ROS1 tyrosine kinase inhibitor (TKI), has demonstrated high and durable response rates, high intracranial objective response rate (ORR), prolonged progression-free survival (PFS), and activity against G2032R with a favorable safety profile. We report outcomes from the pivotal TRUST-I study (ClinicalTrials.gov identifier: NCT04395677 ) of taletrectinib for ROS1+ non–small cell lung cancer in China.

METHODS:

TRUST-I evaluated TKI-naїve and crizotinib-pretreated patients. The primary end point was confirmed ORR (cORR) by independent review committee; key secondary end points included duration of response (DOR), PFS, and safety.

RESULTS:

As of November 2023, 173 patients were enrolled (median age, 55 years; 58% female; 73% never smoked; TKI naїve: n = 106; crizotinib pretreated: n = 67). In TKI-naїve patients, cORR and intracranial cORR were 91% and 88%, respectively, and 52% and 73% in crizotinib-pretreated patients. In TKI-naїve patients, median DOR and median PFS were not reached (NR) with 22.1-month and 23.5-month follow-up, respectively. In crizotinib-pretreated patients, the median DOR was 10.6 months (95% CI, 6.3 months to NR; 8.4-month follow-up), and the median PFS was 7.6 months (95% CI, 5.5 to 12.0 months; 9.7-month follow-up). Eight of 12 patients (67%) with G2032R mutations responded. The most frequent treatment-emergent adverse events (TEAEs) were increased AST (76%), diarrhea (70%), and increased ALT (68%), most of which were grade 1-2. Incidences of neurologic TEAEs were low (dizziness: 23%; dysgeusia: 10%) and mostly grade 1. Discontinuations (5%) and dose reductions (19%) due to TEAEs were low.

CONCLUSION:

Taletrectinib continues to show high and durable overall responses, prolonged PFS, robust activity against intracranial lesions and acquired resistance mutations including G2032R, and a favorable safety profile with a low incidence of neurologic TEAEs.

News (Medical) associated with Taletrectinib

03 Jan 2025

·www.prnewswire.com

Innovent Announces Second New Drug Application of DOVBLERON ® (Taletrectinib Adipate Capsule, ROS1 Inhibitor) was Approved by China's National Medical Products Administration

SAN FRANCISCO and SUZHOU, China, Jan. 2, 2025 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high quality medicines for the treatment of oncology, cardiovascular and metabolic, autoimmune, ophthalmology and other major diseases, today announced that China's National Medical Products Administration (NMPA) has approved the second New Drug Application (NDA) of DOVBLERON® (taletrectinib adipate capsule), a next-generation ROS1 tyrosine kinase inhibitor (TKI), for the treatment of adult patients with locally advanced or metastatic ROS1-positive NSCLC. The approval is based on positive results from the pivotal Phase 2 TRUST-I trial (NCT04395677), a multicenter, open-label, single-arm trial that evaluated the safety, tolerability and efficiency of taletrectinib in Chinese patients with advanced ROS1-positive NSCLC. The findings, presented at the 2024 American Society of Clinical Oncology (ASCO) Annual Meeting and published in the Journal of Clinical Oncology (JCO), demonstrated that taletrectinib continued to show high and durable overall responses and robust activity against intracranial lesions. In ROS1 TKI-naïve (n=106) patients, confirmed objective response rate (cORR, as assessed by an independent review committee, IRC) and intracranial cORR reached as high as 91% and 88%, respectively. After median follow-up of 23.5 months in TKI-naïve patients, median duration of response (IRC-assessed) and median progression-free survival (IRC-assessed) were not reached. [Link] In December 2024, DOVBLERON® was approved by the NMPA for the treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC) who have been previously treated with ROS1 TKIs. DOVBLERON® is the 13th addition to Innovent's commercial portfolio, representing an innovative precision therapy expected to benefit more lung cancer patients alongside our strong TKI franchise. Caicun Zhou, M.D., Ph.D., Director of the Department of Oncology at Shanghai East Hospital, Tongji University, commented: "We are glad to see that DOVBLERON® has been approved for ROS1-positive NSCLC across treatment lines at a fast pace. DOVBLERON® demonstrated superior efficacy compared to the first-generation TKIs. These TRUST-I results reinforce taletrectinib's high overall response and prolonged PFS. The efficacy and safety profile of DOVBLERON® offers a more effective first-line treatment option and I look forward to its benefit in the ROS1-positive NSCLC patients in China." Dr. Hui Zhou, Senior Vice President of Innovent, stated: "The two NDAs approval of DOVBLERON® is a reflection of its potential best-in-class efficacy to fulfill the urgent need of patients with ROS1-positive NSCLC. We recently just launched the first batch of DOVBLERON® to market, rapidly bringing this precision therapy to NSCLC patients who need novel treatment options. Innovent's robust TKI product pipeline—including RETSEMOV®, PEMAZYRE®, DUPERT® and DOVBLERON®—showcases our leadership and synergistic strengths in precision oncology. We endeavor to advance more innovative medicines to enhance patients' quality of life." About ROS1-positive Non-small Cell Lung Cancer Lung cancer continues to have one of the highest global incidences and mortality rates, with NSCLC accounting for about 85% of all cases. In China, it is estimated that approximately 2.6% of patients living with NSCLC are ROS1-positive[i]. Despite recent progress for patients with ROS1-positive NSCLC, there remains a need for more effective and tolerable treatment options. In patients with metastatic ROS1-positive NSCLC that progressed following initial treatment, many have tumors spread to their brain (up to 55%) or acquired resistance mutations, including G2032R. Next-generation ROS1 TKIs demonstrated robust intracranial and G2032R activity. In the clinical management of ROS1-positive NSCLC patients, the first-line application of the new generation ROS1 TKIs can bring a prolonged progression-free survival and provide patients with greater survival benefits. About DOVBLERON ® (Taletrectinib Adipate Capsule) DOVBLERON® is an oral, potent, central nervous system-active, selective, next-generation ROS1inhibitor. Taletrectinib, the active ingredient in DOVBLERON® is being evaluated for the treatment of patients with advanced ROS1-positive NSCLC in two Phase 2 single-arm pivotal studies: TRUST-I (NCT04395677) in China, and TRUST-II (NCT04919811), a global study. DOVBLERON® was approved by China's National Medical Products Administration (NMPA): 1) for the treatment of adult patients with locally advanced or metastatic ROS1-positive NSCLC who have previously been treated with ROS1 TKIs; 2) for the treatment of adult patients with locally advanced or metastatic ROS1-positive NSCLC. Taletrectinib has been granted Orphan Drug Designation by the U.S. FDA for the treatment of patients with ROS1-positive NSCLC and other NSCLC indications, and Breakthrough Therapy Designations by both the U.S. FDA and China's NMPA for the treatment of patients with locally advanced or metastatic ROS1-positive NSCLC. Based on pooled results of the TRUST-I and TRUST-II clinical studies, Nuvation Bio Inc. (NYSE: NUVB) submitted an NDA for taletrectinib to the U.S. FDA for the treatment of patients with advanced ROS1-positive NSCLC (line agnostic, full approval). This NDA was accepted by the U.S. FDA for priority review in December 2024. In June 2021, Innovent and AnHeart Therapeutics (Hangzhou) Co. Ltd., a Nuvation Bio Inc. company, entered into an exclusive license agreement for the co-development and commercialization of taletrectinib in Greater China, including mainland China, Hong Kong, Macau and Taiwan. About Innovent Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that target some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has launched 13 products in the market. It has 4 new drug applications under regulatory review, 3 assets in Phase III or pivotal clinical trials and 17 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Eli Lilly, Sanofi, Incyte, Adimab, LG Chem and MD Anderson Cancer Center. Guided by the motto, "Start with Integrity, Succeed through Action," Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit , or follow Innovent on Facebook and LinkedIn. Forward-Looking Statements This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", "intend" and similar expressions, as they relate to Innovent, are intended to identify certain of such forward-looking statements. Innovent does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections and understandings of the management of Innovent with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties and other factors, some of which are beyond Innovent's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, Innovent's competitive environment and political, economic, legal and social conditions. References [i] Zhang et al. Prevalence of ROS1 fusion in Chinese patients with non-small cell lung cancer. Thorac Cancer. 2019 Jan;10(1):47-53. SOURCE Innovent Biologics WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Orphan DrugDrug ApprovalLicense out/inPhase 2Breakthrough Therapy

23 Dec 2024

·www.businesswire.com

U.S. Food and Drug Administration Accepts for Priority Review Nuvation Bio’s New Drug Application for Taletrectinib for the Treatment of Advanced ROS1-positive Non-Small Cell Lung Cancer

NEW YORK--( BUSINESS WIRE )--Nuvation Bio Inc. (NYSE: NUVB), a global biopharmaceutical company tackling some of the greatest unmet needs in oncology, today announced that the U.S. FDA has accepted the company’s NDA for taletrectinib, an investigational next-generation ROS1 tyrosine kinase inhibitor (TKI), for the treatment of advanced ROS1+ NSCLC (line agnostic). The U.S. FDA has granted the application Priority Review and assigned a Prescription Drug User Fee Act (PDUFA) goal date of June 23, 2025. Priority Review designation underscores the significant advancement taletrectinib may offer patients with ROS1+ NSCLC, for which there remains a high unmet need for new treatment options. Taletrectinib previously received Orphan Drug Designation and is the only ROS1 TKI currently in development that has received Breakthrough Therapy Designation from the U.S. FDA for the treatment of patients with locally advanced or metastatic ROS1+ NSCLC who either have or have not previously been treated with ROS1 TKIs. “We are thrilled to reach this important milestone for taletrectinib, a significant step forward for people living with ROS1-positive NSCLC who urgently need new treatment options,” said David Hung, M.D., Founder, President, and Chief Executive Officer of Nuvation Bio. “With data from over 300 patients—the largest ROS1-positive NSCLC dataset to date supporting an original NDA—taletrectinib has demonstrated the potential to deliver durable and meaningful benefits.” Dr. Hung continued, “Since acquiring AnHeart Therapeutics earlier this year, including taletrectinib, we have executed on our plan to advance taletrectinib toward a full U.S. regulatory approval. The FDA’s Priority Review reflects the strength of our clinical data and the promise taletrectinib holds for patients. As we prepare for a launch as early as mid-2025, we’re taking critical steps to establish Nuvation Bio as a commercial oncology organization, reinforcing our commitment to bringing innovative therapies to patients who need them most.” The NDA is based on the pooled results from the pivotal Phase 2 TRUST-I and TRUST-II studies of taletrectinib, which were presented at the European Society of Medical Oncology (ESMO) Congress in September 2024. About Taletrectinib Taletrectinib is an oral, potent, central nervous system-active, selective, next-generation ROS1 inhibitor specifically designed for the treatment of patients with advanced ROS1+ NSCLC. Taletrectinib is being evaluated for the treatment of patients with advanced ROS1+ NSCLC in two Phase 2 single-arm pivotal studies: TRUST-I (NCT04395677) in China, and TRUST-II (NCT04919811), a global study. Taletrectinib has been granted Orphan Drug Designation by the U.S. FDA for the treatment of patients with ROS1+ NSCLC and other NSCLC indications, and Breakthrough Therapy Designations by both the U.S. FDA and China’s National Medical Products Administration (NMPA) for the treatment of patients with locally advanced or metastatic ROS1+ NSCLC. Based on pooled results of the TRUST-I and TRUST-II clinical studies, the U.S. FDA has accepted for Priority Review Nuvation Bio’s NDA for taletrectinib for the treatment of patients with advanced ROS1+ NSCLC (line agnostic, full approval). Based on results of the TRUST-I clinical study, China’s NMPA approved taletrectinib for the treatment of adult patients with locally advanced or metastatic ROS1+ NSCLC who have previously been treated with a ROS1 TKI and has accepted and granted Priority Review Designation to an NDA for patients who have not previously been treated with a ROS1 TKI. Summary of the Pivotal Pooled TRUST-I and TRUST-II Data The pooled efficacy and safety data from the TRUST-I and TRUST-II studies presented at ESMO are as of June 7, 2024; both studies remain ongoing. The ESMO data set includes 337 patients with advanced ROS1+ NSCLC who received 600mg of taletrectinib orally once daily in 21-day cycles. The primary endpoint of these registrational studies is confirmed objective response rate (cORR) as assessed by an independent review committee (IRC). Key secondary endpoints include intracranial cORR, duration of response (DOR), progression-free survival (PFS), and safety. The Nuvation Bio press release summarizing the pooled results can be viewed here . About ROS1+ NSCLC Each year, more than one million people globally are diagnosed with NSCLC, the most common form of lung cancer. It is estimated that approximately 2% of people with NSCLC have ROS1+ disease. Up to 35% of people newly diagnosed with metastatic ROS1+ NSCLC have tumors that spread to their brain, increasing up to 55% for those whose cancer has progressed following initial treatment. Despite recent progress for people with ROS1+ NSCLC, there remains a need for more effective and tolerable treatment options. About Nuvation Bio Nuvation Bio is a global biopharmaceutical company tackling some of the greatest unmet needs in oncology by developing differentiated and novel product candidates. Nuvation Bio’s portfolio of development candidates includes taletrectinib (ROS1), safusidenib (mIDH1), NUV-1511 (DDC), and NUV-868 (BET). Nuvation Bio was founded in 2018 by biopharma industry veteran David Hung, M.D., who previously founded Medivation, Inc., which brought to patients one of the world’s leading prostate cancer medicines. Nuvation Bio has offices in New York, San Francisco, Boston, and Shanghai. For more information, please visit www.nuvationbio.com or follow us on LinkedIn and X (@nuvationbioinc) . Forward Looking Statements Certain statements included in this press release that are not historical facts are forward-looking statements for purposes of the safe harbor provisions under the United States Private Securities Litigation Reform Act of 1995. Forward-looking statements are sometimes accompanied by words such as “believe,” “may,” “will,” “estimate,” “continue,” “anticipate,” “intend,” “expect,” “should,” “would,” “plan,” “predict,” “potential,” “seem,” “seek,” “future,” “outlook” and similar expressions that predict or indicate future events or trends or that are not statements of historical matters. These forward-looking statements include, but are not limited to, our expectations regarding the timing of FDA approval and commercial launch, a full NDA approval for taletrectinib for the treatment of advanced ROS1+ NSCLC (line agnostic), our expectations of establishing a commercial organization, and taletrectinib’s best-in-class therapeutic potential in advanced ROS1+ NSCLC. These statements are based on various assumptions, whether or not identified in this press release, and on the current expectations of the management team of Nuvation Bio and are not predictions of actual performance. These forward-looking statements are subject to a number of risks and uncertainties that may cause actual results to differ from those anticipated by the forward-looking statements, including but not limited to the challenges associated with conducting drug discovery and initiating or conducting clinical studies due to, among other things, difficulties or delays in the regulatory process, enrolling subjects or manufacturing or acquiring necessary products; the emergence or worsening of adverse events or other undesirable side effects; risks associated with preliminary and interim data, which may not be representative of more mature data; and competitive developments. Risks and uncertainties facing Nuvation Bio are described more fully in its Form 10-Q filed with the SEC on November 6, 2024, under the heading “Risk Factors,” and other documents that Nuvation Bio has filed or will file with the SEC. You are cautioned not to place undue reliance on the forward-looking statements, which speak only as of the date of this press release. Nuvation Bio disclaims any obligation or undertaking to update, supplement or revise any forward-looking statements contained in this press release.

NDAOrphan DrugPhase 2Priority ReviewBreakthrough Therapy

23 Dec 2024

·endpts.com

PDUFAs for Tonix and Nuvation; Sanofi vaccine partnership; RAPT allergy deal

Tonix Pharmaceuticals has received a PDUFA date of Aug. 15, 2025 , for its non-opioid pain drug for the treatment of fibromyalgia. It claims the drug, TNX-102 SL, would be a first-in-class treatment for the condition. The experimental compound has faced repeated setbacks , but in 2023 reported a successful Phase 3 trial that let it go to the FDA. — Drew Armstrong Nuvation Bio also got a PDUFA date of June 23, 2025, for its cancer drug taletrectinib, for patients with advanced ROS1-positive non-small cell lung cancer. Earlier this year, the biotech reported Phase 2 data showing that the drug shrank tumors in 89% of patients. — Drew Armstrong Sanofi will launch and Phase 3 pneumococcal vaccine study with Korea’s SK bioscience . The experimental vaccine is the first to cover more than 20 serotypes that will be tested in a Phase 3 study of young kids, Sanofi said Monday , and more than 7,700 infants, toddlers, young children and adolescents are set to be enrolled. Sanofi and SK are also expanding their partnership, with both companies sharing research and development costs and Sanofi paying $52 million (€50 million) plus potential milestone payments for ex-South Korean commercial rights. — Max Bayer The South San Francisco biotech RAPT Therapeutics will pay $35 million upfront and up to $672.5 million in biobucks to Shanghai Jemincare Pharmaceutical in exchange for the ex-China exclusive license to a half-life extended IgE monoclonal antibody. The drug is in multiple Phase 2 trials in China. RAPT said it plans to first test RPT904 in food allergy next year. — Kyle LaHucik

Phase 3VaccinePhase 2License out/inClinical Result

100 Deals associated with Taletrectinib

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Reactive oxygen species 1 positive non-small cell lung cancer	CN	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	17 Dec 2024

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
CDH1 Mutation Invasive Lobular Breast Carcinoma	Phase 2	US	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	01 Apr 2025
Metastatic breast cancer	Phase 2	US	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	01 Apr 2025
Advanced Lung Non-Small Cell Carcinoma	Phase 2	CN	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	07 Jul 2020
metastatic non-small cell lung cancer	Phase 2	CN	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	07 Jul 2020
Advanced Malignant Solid Neoplasm	Phase 1	JP	Daiichi Sankyo Co., Ltd.	10 Feb 2016
Metastatic Solid Tumor	Phase 1	US	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	01 Sep 2014

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04395677 \| NCT04919811 (TRUST-II, ESMO_ASIA2024) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 Positive	-	Taletrectinib (TKI naive)	iojyllvdag(wnldsraron): HR = 0.76 (95% CI, 0.404 - 1.438) View more	Positive	07 Dec 2024
				Repotrectinib (TKI naive)
NCT04395677 \| NCT04919811 (TRUST-II, ESMO2024) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer Second line \| First line ROS1 Positive	331	Taletrectinib 600 mg QD	wuyihgrvmx(nsykliwmac) = gruaxevscd jkkoeihqla (manxirpbhw ) View more	Positive	14 Sep 2024
				Taletrectinib Taletrectinib 600 mg QD (1 prior ROS1 TKI)	wuyihgrvmx(nsykliwmac) = strphdjhcj jkkoeihqla (manxirpbhw, 10.4 - 31.8) View more
NCT04395677 (TRUST-I, Literature) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer Second line \| First line ROS1 Positive	173	Taletrectinib (TKI naїve)	vyrddcposx(voyrbfsbhk) = mfkiaxxqxu dogsdwbpao (fdkrraycnl ) View more	Positive	01 Jun 2024
				Taletrectinib (crizotinib pretreated)	vyrddcposx(voyrbfsbhk) = yknwcefszd dogsdwbpao (fdkrraycnl ) View more
NCT04395677 (TRUST-I, Pubmed \| J Clin Oncol)	Phase 2	Non-Small Cell Lung Cancer ROS1+	173	Taletrectinib	nozwehqacp(aaoukxvzsk) = tzdliuhiol bzgwcuerrk (rgepicrifr ) View more	Positive	01 Jun 2024
				Crizotinib	nozwehqacp(aaoukxvzsk) = jdszokbsll bzgwcuerrk (rgepicrifr ) View more
NCT04395677 (TRUST-I, ASCO2024) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 G2032R	173	Taletrectinib	zyphssozon(sgofvajxsd) = xaglyancsd hetyrwltfm (gaexqvhcii, 83 - 95) View more	Positive	24 May 2024
				Chemotherapy	zyphssozon(sgofvajxsd) = pnfsdkoisf hetyrwltfm (gaexqvhcii, 40 - 65) View more
NCT04919811 (TRUST-II, ESMO2023) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 Positive	46	Taletrectinib (NSCLC: ROS1 TKI-naive, ≤1 line of chemotherapy (CT))	jpqgqtsqaa(didmutsypv) = dkwqtkyukn cepiirfdwe (hibxzaprol ) View more	Positive	23 Oct 2023
				Taletrectinib (NSCLC: 1 prior ROS1 TKI, ≤1 line of CT)	jpqgqtsqaa(didmutsypv) = rvaldfrkfi cepiirfdwe (hibxzaprol ) View more
NCT04395677 (TRUST-I, ESMO_ELCC2023) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 Positive	109	Taletrectinib, 600mg QD (ROS1 TKI-Naïve)	masjlnjvqj(xxlzqbanyi) = wgtncmzayf akjbweiekr (jvcoqngmwa, 83.4 - 97.5) View more	Positive	31 Mar 2023
NCT04395677 (TRUST, ASCO2022) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 Positive \| G2032 Mutation	86	Taletrectinib 600mg (TKI -naïve cohort)	rqdugatbzm(muxntxiwbz) = qorjshpwzv hjccnovwlk (grncmrnbcn, 83.1 - 99.4) View more	Positive	02 Jun 2022
				Taletrectinib 600mg (crizotinib-pretreated cohort)	rqdugatbzm(muxntxiwbz) = juuvmzxhkd hjccnovwlk (grncmrnbcn, 52.8 - 91.8) View more
NCT04395677 (TRUST, ASCO2021)	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer	22	Taletrectinib 400 mg QD	ddglpllulh(jwhygpxvmh) = jjyuoducch ccqbvpbjfa (ruvuqjuszz, 72% - 100%) View more	Positive	28 May 2021
				Taletrectinib 600 mg QD	rmezdobnlx(cpbcfscjcs) = wwryhafwav znsuamoceo (emdksgaeau ) View more
NCT02279433 (Pubmed \| Clin Cancer Res) Manual	Phase 1	HR-positive/HER2-low Solid Tumors	46	Taletrectinib	cccfuboxhj(giglqveidg) = grade 3 transaminases increase occurred in two patients (1,200-mg once-daily dose) oejeabhrlu (sezrrnhcpq ) View more	Positive	15 Sep 2020

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