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 cancerLocally Advanced 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

AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup

Nuvation Bio, Inc.

Asymchem Life Science Tianjin Co. Ltd.

+ [1]

Inactive Organization

Daiichi Sankyo Co., Ltd.

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationPriority Review (CN), Breakthrough Therapy (CN), Breakthrough Therapy (US), Orphan Drug (US)

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 Oct 2024

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 ; Song, Xiaoling ; Qu, Xiaojuan ; Zhu, Qiaoliang ; Wei, Yongqi ; Lu, Chunlai ; Ge, Di ; 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

08 Oct 2024

·www.prnewswire.com

Innovent and Ask Pharm Announce Strategic Collaboration for Limertinib, a Third-generation EGFR TKI for the Treatment of Lung Cancer

SAN FRANCISCO and SUZHOU, China, Oct. 7, 2024 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of oncologic, autoimmune, cardiovascular and metabolic, ophthalmologic and other major diseases, and Jiangsu Aosaikang Pharmaceutical Co. Ltd. (ASK Pharm, 002755.SZ), announced that the two parties have entered into a strategic collaboration regarding limertinib, a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) for the treatment of lung cancer. Under the agreement, Innovent will obtain the exclusive commercialization rights for limertinib in mainland China, and will be entitled to receive a commercialization service fee based on the product's net sales in the region. Ask-Pharm as the MAH holder, will be responsible for the production and commercial supply of limertinib and will be eligible for upfront, regulatory and sales milestone payments. Limertinib is an orally administrated, third-generation novel EGFR TKI with proprietary rights. Two New Drug Applications (NDAs) for limertinib have been accepted and are under review by China's National Drug Administration (NMPA): (1) for the treatment of adult patients with locally advanced or metastatic EGFR T790M mutation-positive NSCLC, confirmed by a validated diagnostic test, whose disease has progressed after EGFR TKI therapy; and (2) for the first-line treatment of adult patients with locally advanced or metastatic NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations. In a multi-center, randomized, double-blind, controlled Phase 3 clinical trial, limertinib's efficacy and safety were compared with gefitinib in the first-line treatment of patients with locally advanced or metastatic NSCLC with EGFR mutations. The Phase 3 clinical trial met its primary endpoint, and detailed data and analysis will be presented at future academic conferences or published in academic journals. Previously, results of limertinib from a Phase 2b clinical study were presented in a poster session at the 2022 American Society of Clinical Oncology (ASCO) Annual Meeting. Dr. Michael Yu, Founder, Chairman and CEO of Innovent, stated: "We are delighted to enter this strategic collaboration with ASK Pharm, one of the most innovative biopharmaceutical companies in China, which will further strengthen Innovent's leadership in oncology. Together with our partners, Innovent has successfully developed a series of high-quality innovative medicines for lung cancer treatments, including TYVYT® (sintilimab Injection), BYVASDA® (bevacizumab Injection), Retsevmo® (selpercatinib), Dupert® (fulzerasib) and Taletrectinib (ROS1 Inhibitor, NDA under review). The addition of limertinib will offer a valuable new treatment option for Chinese patients with EGFR-mutated lung cancer. Innovent remains committed to investing in innovation and collaborative partnerships, aiming to enhancing the accessibility and affordability of innovative therapies in China to benefit even more patients." Mr. Jingfei Ma, Director and General Manager of ASK Pharm, stated: "We are pleased to form a strategic partnership with Innovent Biologics. Oncology is one of the four core areas of focus for ASK Pharm, and our oncology product line spans chemotherapy drugs, small molecule targeted drugs, and biologics. Limertinib, ASK Pharm's first innovative drug, targets the cancer type with the highest incidence and mortality rates in China. Focused on addressing the most common mutations in lung cancer, Ask-Pharm is committed to providing effective drugs for the vast number of patients with EGFR-mutated lung cancer. Innovent has a rich product pipeline in the field of lung cancer, which can form advantageous synergies with limertinib. In addition, with Innovent's professional and efficient marketing team and proven commercialization capabilities, we are confident that this cooperation will help limertinib to fully realize its clinical value, so that more patients can benefit from it." About EGFR mutation-positive non-small-cell lung cancer (NSCLC) Lung cancer is the leading cause of cancer-related death and the second more common cancer worldwide. In China, it has both the highest incidence and mortality rates among malignant tumors. Non-small cell lung cancer (NSCLC) accounts for approximately 80% to 85% of all lung cancers, and approximately 70% of NSCLC patients are diagnosed with locally advanced or metastatic disease that is not eligible to surgical resection. EGFR is the most frequent driver mutation in NSCLC, with 30% to 50% of Asian NSCLC patients having EGFR mutations. EGFR-TKIs are the recommended first-line standard of care for this group, with third-generation EGFR inhibitors offering the broadest applicability. About Limertinib Limertinib is an orally-administrated, third-generation EGFR TKI with proprietary rights, classified as a new molecular entity. Two New Drug Applications (NDAs) of limertinib are currently under review by China's National Drug Administration (NMPA): (1) for the treatment of adult patients with locally advanced or metastatic EGFR T790M mutation-positive NSCLC, confirmed by an approved test, whose disease has progressed following EGFR TKI therapy; and (2) for the first-line treatment of adult patients with locally advanced or metastatic NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations. In a multi-center, randomized, double-blind, controlled Phase 3 clinical trial, the efficacy and safety of limertinib were compared to gefitinib in the first-line treatment of patients with locally advanced or metastatic NSCLC harboring EGFR mutations. The Phase 3 clinical trial met its primary endpoint, and the results will be presented at future academic conferences or published in academic journals. Results from a Phase 2b clinical study were presented in a poster session at the 2022 American Society of Clinical Oncology (ASCO) Annual Meeting. In October 2024, Innovent and ASK Pharm entered into a strategic collaboration and license agreement regarding limertinib in mainland China. 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 11 products in the market. It has 5 new drug applications (NDA) under regulatory review, 3 assets in Phase III or pivotal clinical trials and 18 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. About Jiangsu Aosaikang Pharmaceutical Co. Ltd. (ASK Pharm) Founded in January 2003, Jiangsu Aosaikang Pharmaceutical Co. Ltd. (ASK Pharm) is a research-based pharmaceutical enterprise that integrates and streamlines innovative research and development with manufacture, marketing promotion and sales of proprietary pharmaceuticals, fine chemicals and health-care products. ASK Pharm specializes in digestive disease, multidrug resistant infection, oncology and chronic disease areas. ASK Pharm focuses on the R&D of small-molecule targeted innovative drugs and immuno-oncology biologic drugs. Currently, there are 48 major research projects, including 11 disclosed key projects focused on innovative chemical and biologic drugs. Among these, the innovative anti-tumor drug Limertinib are in the NDA stage, while ASKC109 (maltol iron capsules) and ASKB589 (Claudin18.2 monoclonal antibody) are in Phase III clinical trials. ASK Pharm has Ranked among the top 20 best industrial enterprises in China's pharmaceutical R&D pipeline for 14 consecutive years and it has also received numerous honors such as "Top Ten National R&D Innovators", "Best National Enterprise for Investment", and "National Torch Program High-Tech Enterprises". For more information, visit . Innovent's 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. Innovent, the Directors and the employees of Innovent assume (a) no obligation to correct or update the forward-looking statements contained in this site; and (b) no liability in the event that any of the forward-looking statements does not materialize or turn out to be incorrect. 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

Phase 2Phase 3License out/inClinical ResultNDA

08 Oct 2024

·www.pharmaceutical-technology.com

Innovent and ASK Pharm to commercialise limertinib for lung cancer

Limertinib is intended for the treatment of patients with lung cancer. Credit: New Africa/Shutterstock. Innovent Biologics and Jiangsu Aosaikang Pharmaceutical (ASK Pharm) have signed a strategic partnership agreement for the commercialisation of limertinib to treat lung cancer. Limertinib is an orally administrated third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). This collaboration will grant Innovent exclusive rights to commercialise the asset within mainland China, and entitles the company to a service fee based on net sales. ASK Pharm will serve as the marketing authorisation holder and will oversee the manufacturing and commercial distribution of the product. ASK Pharm is entitled to upfront payments and milestone payments contingent on meeting regulatory and sales goals. See Also: Activist investor Starboard forges $1bn stake in Pfizer to swing profits Healthcare Payers for the Pharmaceutical Industry Two new drug applications for limertinib are currently under review by China’s National Medical Products Administration. One application is for an indication to treat adults with locally advanced or metastatic EGFR T790M mutation-positive non-small cell lung cancer (NSCLC), post-EGFR TKI therapy progression. The other is for the first-line treatment of NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations in adults. The efficacy and safety of limertinib were evaluated in a randomised, multicentre, double-blind, controlled Phase III clinical trial comparing it to gefitinib for the first-line treatment of patients with locally advanced or metastatic NSCLC with EGFR mutations. The trial successfully met its primary endpoint, indicating a potential new option for patients with this form of lung cancer. Innovent founder, chairman and CEO Dr Michael Yu stated: “We are delighted to enter this strategic collaboration with ASK Pharm, one of the most innovative biopharmaceutical companies in China, which will further strengthen Innovent’s leadership in oncology. “Together with our partners, Innovent has successfully developed a series of high-quality innovative medicines for lung cancer treatments, including TYVYT (sintilimab Injection), BYVASDA (bevacizumab Injection), Retsevmo (selpercatinib), Dupert (fulzerasib) and Taletrectinib (ROS1 Inhibitor). “The addition of limertinib will offer a valuable new treatment option for Chinese patients with EGFR-mutated lung cancer.” In August 2024, the company’s Kristen rat sarcoma G12C inhibitor, Dupert (fulzerasib), received China’s National Medical Products Administration (NMPA) approval to treat advanced non-small cell lung cancer (NSCLC) in adults.

License out/inPhase 3Drug ApprovalCSCO

14 Sep 2024

·endpts.com

Nuvation Bio to head to FDA with pooled ROS1-positive lung cancer data

Nuvation Bio outlined pooled data from its two Phase 2 studies at the annual European Society for Medical Oncology confab in Barcelona this weekend as it prepares to approach the FDA soon. The company said that across the two trials — one conducted in China, the other in Western countries — 89% of patients saw their tumors shrink after taking its once-daily oral drug taletrectinib. Separate datasets from both Phase 2 studies, as well as the pooled ESMO analysis, are expected to form the backbone of Nuvation’s FDA submission, CEO David Hung told Endpoints News . With the data, Nuvation is aiming to capitalize on its all-stock deal for AnHeart Therapeutics from March. Nuvation enrolled 337 patients who had ROS1-positive non-small cell lung cancer in both studies, and individuals took 600 mg of the drug in 21-day cycles. The median follow-up was 21 months, and the cut-off date was June 7. Researchers also took a closer look at 160 patients who hadn’t yet received TKI inhibitors in the studies. Nuvation said tumors shrank in 89% of these individuals, and measurable brain metastases shrank in 13 of 17 people. The median duration of response was 44 months and median progression-free survival was 46 months, Nuvation said. Additionally, 56% of 113 patients who had previously received a TKI inhibitor also saw their tumors shrink. The brain metastases shrank in 21 of 32 patients as well. Hung said that these groups of patients are important to the FDA because ROS1-positive NSCLC is much rarer and more aggressive than ROS1-negative NSCLC. TKI inhibitors are approved to treat the ROS1-positive form, but many patients end up developing resistance mutations to them. “This is a relatively rare type of lung cancer. It’s about 2% of non-small cell lung cancer, but it tends to be quite aggressive,” Hung said. “If you look at the standard of care for non-small lung cancer in immuno-oncology agents and chemotherapy, the median progression-free survival is generally about six to eight months.” Analysts also viewed the data positively after the Western study data were published at the World Conference on Lung Cancer annual meeting earlier this week. TD Cowen analyst Yaron Werber wrote that the WCLC data “continue to support taletrectinib’s promise” in ROS1-positive NSCLC. If everything goes according to plan, Werber expects Nuvation could launch taletrectinib by the end of 2025. Hung is also experienced in running biotechs attractive to large pharma M&A teams — in 2016, Pfizer acquired Hung’s last biotech, Medivation, for $14 billion.

Phase 2AcquisitionClinical Result

100 Deals associated with Taletrectinib

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Reactive oxygen species 1 positive non-small cell lung cancer	NDA/BLA	CN	Asymchem Life Science Tianjin Co. Ltd.	22 Nov 2023
Reactive oxygen species 1 positive non-small cell lung cancer	NDA/BLA	CN	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	22 Nov 2023
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 3	-	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	01 Sep 2024
CDH1 Mutation Invasive Lobular Breast Carcinoma	Phase 2	US	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	01 Oct 2024
Metastatic breast cancer	Phase 2	US	AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup	01 Oct 2024
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.	01 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, 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 (TKI naive)	ktnikfscax(qrxhrdvmog) = ffvvyuovnt nxnkcpscul (tsljuxnzgz ) View more	Positive	14 Sep 2024
				Taletrectinib 600 mg QD (1 prior ROS1 TKI)	ktnikfscax(qrxhrdvmog) = srwyfhrjwx nxnkcpscul (tsljuxnzgz, 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)	ztrevhottd(awldcxjwpz) = nfrdkhdvzo izrbaogrvq (wgworcfjll ) View more	Positive	01 Jun 2024
				Taletrectinib (crizotinib pretreated)	ztrevhottd(awldcxjwpz) = pjckejqxjl izrbaogrvq (wgworcfjll ) View more
NCT04395677 (TRUST-I, Pubmed \| J Clin Oncol)	Phase 2	Non-Small Cell Lung Cancer ROS1+	173	Taletrectinib	esqdvpzdzp(wyygqmdwss) = ifqyaetjsp wdpxagqstp (cjmepnlsnk ) View more	Positive	01 Jun 2024
				Crizotinib	esqdvpzdzp(wyygqmdwss) = qyevgrxkcn wdpxagqstp (cjmepnlsnk ) View more
NCT04395677 (TRUST-I, ASCO2024) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 G2032R	173	Taletrectinib (TKI-Naïve)	ifpovlosuh(bfvibejfsv) = pjbcekdcdt rhunawjeqe (drfltsfxgc, 83 - 95) View more	Positive	24 May 2024
				taletrectinib (TKI-Pretreated)	ifpovlosuh(bfvibejfsv) = ozocnovalr rhunawjeqe (drfltsfxgc, 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))	sfmzpnaasr(ffhgzapees) = wehhrllued ijogwqyfwp (zrptuaukuk ) View more	Positive	23 Oct 2023
				Taletrectinib (NSCLC: 1 prior ROS1 TKI, ≤1 line of CT)	sfmzpnaasr(ffhgzapees) = ddnnlcidau ijogwqyfwp (zrptuaukuk ) 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	ayzdhlnqal(zzzfbttimp) = nldtqmutlc mmmflabdnw (oaooucmmnx ) View more	Positive	31 Mar 2023
				Taletrectinib, 600mg QD (ROS1 TKI-Naïve)	ayzdhlnqal(zzzfbttimp) = xsnvxedmvv mmmflabdnw (oaooucmmnx, 83.4 - 97.5) View more
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)	swzocszdmm(pfskbgdpot) = fcmnbsqmav hetulnxmgy (csaujzzlqz, 83.1 - 99.4) View more	Positive	02 Jun 2022
				Taletrectinib 600mg (crizotinib-pretreated cohort)	swzocszdmm(pfskbgdpot) = fssyiaeyry hetulnxmgy (csaujzzlqz, 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	hdfqwnvjcs(nmbgyrdcbs) = rucntescjz jbvbeieebe (ppcokqrohk, 72% - 100%) View more	Positive	28 May 2021
				Taletrectinib 600 mg QD	ykpngilwah(fueqstjtpg) = ttibpvzisu oagslyqpkt (dkcbsgeqtx ) View more
NCT02279433 (Pubmed \| Clin Cancer Res) Manual	Phase 1	HR-positive/HER2-low Solid Tumors	46	Taletrectinib	bvpezgfymn(vpbrtaifuk) = grade 3 transaminases increase occurred in two patients (1,200-mg once-daily dose) skzvypdtpf (hstriafmmr ) View more	Positive	15 Sep 2020
NCT02279433 (ASCO2018)	Phase 1	HR-positive/HER2-low Solid Tumors	35	DS-6051b	ltdvccfkut(ndvwlgrchz) = vwpauppoaj mpwzxxhtvy (arqbjrrbgu ) View more	-	01 Jun 2018

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Taletrectinib

Overview

Basic Info

Structure

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation