RegulationOrphan Drug (United States), Priority Review (China), Breakthrough Therapy (China), Conditional marketing approval (China), Priority Review (United States), Breakthrough Therapy (United States)

Structure/Sequence

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

/ 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 Date27 Nov 2024

Sponsor / Collaborator

Nuvation Bio, Inc.

[+1]

CTR20222707

/ CompletedPhase 1

在中国健康男性成人中的一项I期，单中心，开放，固定序列的研究评估奥美拉唑对AB-106药代动力学的影响

[Translation] A phase I, single-center, open-label, fixed-sequence study evaluating the effect of omeprazole on the pharmacokinetics of AB-106 in healthy Chinese male adults

评估在健康成人受试者中多剂量奥美拉唑镁肠溶片对单剂量 AB-106 胶囊给药后 PK 暴露参数的影响

[Translation]

To evaluate the effects of multiple doses of omeprazole magnesium enteric-coated tablets on PK exposure parameters following a single dose of AB-106 capsules in healthy adult subjects

Start Date02 Nov 2022

Sponsor / Collaborator

AnHeart Therapeutics (Hangzhou) Co., Ltd.Startup

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 ; Fan, Huijie ; Wang, Xicheng ; Lovly, Christine M. ; Yan, Bing ; Liu, Yunpeng ; Ren, Yizhong ; Zhou, Caicun ; Zhao, Yanqiu ; 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

12 Mar 2025

·www.prnewswire.com

ROZLYTREK's Market Growth Reflects Transforming Treatment for NTRK and ROS1-Positive Cancers | DelveInsight

As biomarker testing and the demand for tumor-agnostic therapies rise, ROZLYTREK can potentially target a specialized yet valuable market segment. While competition from other TRK inhibitors, such as larotrectinib (VITRAKVI), may influence growth, its ability to penetrate the CNS provides a distinct advantage. LAS VEGAS, March 12, 2025 /PRNewswire/ -- DelveInsight's " ROZLYTREK Market Size, Forecast, and Market Insight Report" highlights the details around ROZLYTREK, an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1, and ALK with IC50 values of 0.1 to 2 nM. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of ROZLYTREK. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. Roche's ROZLYTREK (entrectinib) Overview ROZLYTREK is a tumor-agnostic therapy that introduces a novel approach to cancer treatment. Its active ingredient, entrectinib, inhibits tropomyosin receptor tyrosine kinases (TRKA, TRKB, and TRKC), which are encoded by the NTRK1, NTRK2, and NTRK3 genes. It also targets ROS1 and ALK, with IC50 values ranging from 0.1 to 2 nM, while showing weaker inhibition of JAK2 and TNK2 (IC50 > 5 nM). The primary active metabolite, M5, exhibits similar inhibitory activity against TRK, ROS1, and ALK. Fusion proteins involving TRK, ROS1, or ALK kinase domains can promote tumor growth by excessively activating downstream signaling pathways, leading to uncontrolled cell proliferation. Entrectinib has demonstrated both in vitro and in vivo efficacy in inhibiting cancer cell lines across multiple tumor types carrying NTRK, ROS1, or ALK fusions. Additionally, it achieves steady-state brain-to-plasma concentration ratios between 0.4 and 2.2 in animal studies (mice, rats, and dogs) and has shown anti-tumor effects in mice with intracranial tumors driven by TRKA and ALK. ROZLYTREK is an orally administered, once-daily treatment approved for NTRK fusion-positive solid tumors and ROS1-positive NSCLC in several countries, including Australia, Canada, the EU, Israel, Japan, New Zealand, South Korea, Taiwan, and the US, with additional regulatory reviews ongoing worldwide. The recommended ROZLYTREK dosage for ROS1-positive NSCLC is 600 mg once daily, with or without food, until disease progression or unacceptable toxicity. For NTRK fusion-positive solid tumors, the ROZLYTREK dosage guidelines are as follows: Adults and pediatric patients with a body surface area (BSA) of ≥1.51 m²: 600 mg once daily Pediatric patients older than 6 months: 300 mg/m² to a maximum of 600 mg Pediatric patients between 1 month and 6 months: 250 mg/m² once daily Learn more about ROZLYTREK projected market size for ROS1 NSCLC @ ROZLYTREK Market Potential Receptor Tyrosine Kinase (ROS1) is an essential transmembrane receptor protein that regulates key cellular functions such as apoptosis, survival, differentiation, proliferation, migration, and transformation. It plays a pivotal role in various cancers, including glioblastoma, colorectal cancer, gastric adenocarcinoma, inflammatory myofibroblastic tumor, ovarian cancer, angiosarcoma, and NSCLC. A ROS1 inhibitor is a drug designed to block the activity of abnormal ROS1 fusion proteins present in certain cancer cells. By inhibiting this protein, these inhibitors help restrict cancer cell growth and metastasis. As a type of targeted therapy, ROS1 inhibitors also act on multiple kinases, including Anaplastic Lymphoma Kinase (ALK) and Mesenchymal Epithelial Transition (MET), alongside ROS1. These inhibitors specifically target the kinase domain of ROS1, with conventional kinases classified into DFG-in (active, type I) and DFG-out (inactive, type II) based on their domain structure. For patients with stage IV ROS1-positive NSCLC, treatment with a ROS1 tyrosine kinase inhibitor (TKI) is recommended. ROS1 inhibitors have demonstrated remarkable efficacy in treating NSCLC, encompassing both approved therapies and emerging treatments under development. They have significantly advanced NSCLC management, establishing themselves as a crucial therapeutic approach. The current market for ROS1-positive NSCLC is largely dominated by TKIs such as XALKORI. According to DelveInsight's analysis, the market size for ROS1 inhibitors in NSCLC across the 7MM was valued at approximately USD 290 million in 2023, with the United States contributing the largest share. The market for ROS1 inhibitors is projected to experience substantial growth in the coming years. This expansion is driven by rising biomarker testing rates, a growing number of cancer diagnoses, increased awareness of ROS1 mutations, and the introduction of next-generation ROS1 TKIs. These advanced therapies offer improved CNS penetration and a broader range of coverage against ROS1 resistance mutations compared to first-generation TKIs. Discover more about the ROS1 inhibitors market in detail @ ROS1 Inhibitors Market Report Emerging Competitors of ROZLYTREK The promising ROS1 inhibitors in the pipeline that will give tough competition to Roche's ROZLYTREK include DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Zidesamtinib (NVL-520) (Nuvalent), ANS03 (Avistone Biotechnology), Zanidatamab (Jazz Pharmaceuticals), PT-112 (Promontory Therapeutics), and others. In December 2024, Nuvation Bio announced that the US FDA had granted the application Priority Review and assigned a Prescription Drug User Fee Act (PDUFA) goal date of June 2025. The company is preparing for a launch as early as mid-2025. To know more about the number of competing drugs in development, visit @ ROZLYTREK Market Positioning Compared to Other Drugs Key Milestones of ROZLYTREK In October 2023, the US FDA granted accelerated approval to ROZLYTREK in new oral pellet form for pediatric patients older than 1 month with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory standard therapy. In August 2020, the EC granted conditional marketing authorization for ROZLYTREK for the treatment of adult and pediatric patients 12 years of age and older with solid tumors expressing an NTRK gene fusion, who have a disease that is locally advanced, metastatic, or where surgical resection is likely to result in severe morbidity, and who have not received a prior NTRK inhibitor, who have no satisfactory treatment options. The EC also approved ROZLYTREK for the treatment of adults with ROS1-positive, advanced NSCLC not previously treated with ROS1 inhibitors. In February 2020, Chugai obtained approval for an additional indication of ROZLYTREK for the treatment of ROS1 fusion-positive, unresectable, advanced, or metastatic NSCLC from the MHLW. In September 2019, Chugai Pharmaceutical announced the launch of ROZLYTREK 100 mg and 200 mg capsules, for the treatment of NTRK fusion-positive advanced or recurrent solid tumors. In August 2019, the US FDA approved ROZLYTREK to treat adults with ROS1-positive, metastatic NSCLC. The FDA has also granted accelerated approval to ROZLYTREK for the treatment of adult and pediatric patients 12 years of age and older with solid tumors that have an NTRK gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory alternative therapy. In June 2019, the MHLW approved ROZLYTREK for treating adult and pediatric patients with NTRK fusion-positive, advanced recurrent solid tumors. In February 2019, the US FDA issued a priority review designation letter to ROZLYTREK adult patients with metastatic NSCLC whose tumors are ROS1–positive. In December 2018, ROZLYTREK received ODD in Japan with the intended indication of NTRK fusion-positive, locally advanced, or metastatic solid tumors. In September 2018, ROZLYTREK received SAKIGAKE designation for the treatment of adult and pediatric patients with NTRK gene fusion-positive, locally advanced, or metastatic solid tumors who have progressed following prior therapies or have no acceptable standard therapies. In July 2018, Chugai entered into a license agreement with Roche for entrectinib. Under the terms of the agreement, Chugai obtains exclusive rights for the development and marketing of entrectinib in Japan and will make upfront and milestone payments to Roche. In December 2017, Roche and Ignyta entered a definitive merger agreement for Roche to fully acquire Ignyta for USD 27.00 per share in an all-cash transaction. In October 2017, ROZLYTREK was awarded PRIME status for treating NTRK fusion-positive, locally advanced, or metastatic solid tumors in adult and pediatric patients who have either progressed following prior therapies or have no acceptable standard therapy by EMA. In May 2017, ROZLYTREK was granted BTD for the treatment of NTRK fusion-positive, locally advanced, or metastatic solid tumors in adult and pediatric patients who have either progressed following prior therapies or who have no acceptable standard therapies by the US FDA. In February 2015, the US FDA granted ODD to ROZLYTREK for treating TrkA-positive, TrkB-positive, TrkC-positive, ROS1-positive or ALK-positive NSCLC. Discover how ROZLYTREK is shaping the ROS1 NSCLC treatment landscape @ Roche ROZLYTREK ROZLYTREK Market Dynamics ROZLYTREK competitive positioning in the market is driven by its tumor-agnostic approval, allowing it to cater to multiple rare cancers with a single therapy. The drug has gained regulatory approval in major markets, including the US, Europe, and Japan, benefiting from an increasing emphasis on biomarker-driven oncology treatments. Its key competitor, Bayer's VITRAKVI (larotrectinib), has a similar mechanism of action but differs in pharmacokinetics and tolerability, creating a nuanced competitive landscape. Market adoption of ROZLYTREK is influenced by the growing use of comprehensive genomic profiling (CGP) in oncology, which facilitates the identification of eligible patients with NTRK or ROS1 fusions. However, its commercial success is partially constrained by the rarity of these genetic alterations, which limits the addressable patient population. Additionally, the high cost of precision oncology therapies and reimbursement challenges in certain healthcare systems can impact uptake. Nonetheless, increasing awareness and advancements in diagnostic infrastructure are expected to support market growth. From a strategic perspective, Roche has leveraged partnerships and real-world evidence to expand the drug's adoption. The company is actively working on label expansions and combination strategies to maximize ROZLYTREK's commercial potential. Additionally, the growing use of next-generation sequencing (NGS) panels in routine cancer diagnostics may boost the identification rate of eligible patients, driving future market penetration. The competitive landscape could see further evolution with the potential entry of new TRK/ROS1 inhibitors, particularly next-generation agents designed to address resistance mutations. However, ROZLYTREK's strong clinical efficacy, broad tissue-agnostic approval, and Roche's global oncology expertise position it well in the precision medicine segment. As personalized oncology continues to gain traction, the drug's long-term success will depend on physician awareness, diagnostic advancements, and favorable pricing and reimbursement strategies. Dive deeper to get more insight into ROZLYTREK's strengths & weaknesses relative to competitors @ ROZLYTREK Market Drug Report Table of Contents Related Reports ROS1 Inhibitors Market ROS-1 Inhibitors Market Size, Target Population, Competitive Landscape & Market Forecast – 2034 report deliver an in-depth understanding of the market trends, market drivers, market barriers, and key ROS1 inhibitors companies, including AnHeart Therapeutics, Nuvalent, Bristol Myers Squibb, Genentech, Pfizer, among others. Non-small Cell Lung Cancer Market Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key NSCLC companies including Daiichi Sankyo, AstraZeneca, Gilead Sciences, BieGene, AbbVie, Roche, Merck, Novartis, Pfizer, Takeda Pharmaceuticals, Eli Lilly, BerGenBio, GlaxoSmithKline, Duality biologics, among others. Non-small Cell Lung Cancer Pipeline Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key non-small cell lung cancer companies, including BridgeBio Pharma, Daiichi Sankyo, EMD Serono, Merck, BridgeBio Pharma, Abbvie, Pfizer, Eli Lilly and Company BioNTech SE, Shenzhen TargetRx, Taiho Pharmaceutical, Chong Kun Dang, Bristol Myers Squibb, Innovent Biologics, Xuanzhu Biopharmaceutical, Bayer, GeneScience Pharmaceuticals, InventisBio, Apollomics, Imugene, Ono Pharmaceutical, Pierre Fabre, Jiangsu Hengrui Medicine Co., Bristol-Myers Squibb, Surface Oncology, Inhibrx, Sinocelltech, Mirati Therapeutics, REVOLUTION Medicines, Yong Shun Technology Development, Iovance Biotherapeutics, Galecto Biotech, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalPriority ReviewLicense out/in

06 Mar 2025

·www.prnewswire.com

TEPMETKO Continues to Strengthens its Position as a Leading METex14 Skipping NSCLC Therapy | DelveInsight

With increasing biomarker-driven cancer treatments, TEPMETKO benefits from growing adoption in precision oncology. Competition from other MET inhibitors like TABRECTA (capmatinib) exists, but TEPMETKO's once-daily dosing and efficacy profile offer differentiation. LAS VEGAS, March 6, 2025 /PRNewswire/ -- DelveInsight's " TEPMETKO Market Size, Forecast, and Market Insight Report" highlights the details around TEPMETKO, a kinase inhibitor indicated for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of TEPMETKO. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. EMD Serono's TEPMETKO (tepotinib) Overview TEPMETKO is a kinase inhibitor prescribed for adult patients with metastatic non-small cell lung cancer (NSCLC) carrying MET exon 14 skipping alterations. The active component is Tepotinib (as hydrochloride monohydrate), administered orally. Patients should be cautioned about the heightened risk of severe or fatal interstitial lung disease/pneumonitis, liver toxicity, and potential embryo-fetal toxicity, necessitating effective contraception during and shortly after treatment. Tepotinib specifically targets MET, including variants with exon 14 skipping mutations. It blocks HGF-dependent and independent MET phosphorylation, disrupting MET-driven signaling pathways. Additionally, at clinically relevant concentrations, Tepotinib inhibits melatonin 2 and imidazoline 1 receptors. In vitro studies show that it suppresses tumor cell proliferation, anchorage-independent growth, and migration of MET-dependent cancer cells. In mouse models with MET-driven tumors, including those with MET exon 14 skipping alterations, Tepotinib reduced tumor growth, sustained MET phosphorylation inhibition, and, in one case, decreased metastasis formation. The recommended dose of TEPMETKO is 450 mg taken orally once daily until disease progression or intolerable toxicity occurs. Patients should take it at the same time each day, swallowing tablets whole without chewing, crushing, or splitting them. If a dose is missed and less than eight hours remain until the next scheduled dose, patients should skip it. In cases of vomiting after taking TEPMETKO, the next dose should be taken at the usual time. Learn more about TEPMETKO projected market size for NSCLC @ TEPMETKO Market Potential Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for 81% of all diagnosed cases. Early detection greatly improves outcomes, but diagnosing NSCLC and other lung cancers is challenging because their symptoms are often mistaken for common illnesses or the long-term effects of smoking. Consequently, 80% of NSCLC cases are already at advanced stages by the time they are identified, making treatment more difficult. Around 80% of EGFR mutations in NSCLC involve either exon 19 deletions or the exon 21 L858R substitution, both of which are classified as sensitizing mutations. Until the last decade, chemotherapy was the primary treatment for advanced and metastatic lung cancer. However, this changed in 2015 with the approval of the first immune checkpoint inhibitor (ICI), KEYTRUDA (pembrolizumab), as a second-line therapy for advanced cases. This was followed by TECENTRIQ (atezolizumab) in 2016. Both therapies were later approved for first-line treatment, broadening their use to a larger patient population. In 2020, the combination of OPDIVO (nivolumab) and ipilimumab also received approval as a first-line treatment for metastatic NSCLC. According to DelveInsight, the NSCLC market size across the 7MM is projected to grow from USD 30 billion in 2024, with a substantial CAGR through 2034. This growth is largely driven by the introduction of emerging therapies during the forecast period (2025–2034). Discover more about the NSCLC market in detail @ Non-small Cell Lung Cancer Market Report Emerging Competitors of TEPMETKO The NSCLC pipeline is very robust with the promising therapies such as Telisotuzumab vedotin (AbbVie), Patritumab deruxtecan (Daiichi Sankyo/AstraZeneca), Datopotamab deruxtecan (Daiichi Sankyo/AstraZeneca), Eftilagimod alpha (Immutep), BNT311/GEN1046 (acasunlimab) (Genmab), V940 (mRNA-4157) + Pembrolizumab (Moderna Therapeutics/Merck), Plinabulin + Docetaxel (BeyondSpring), Olomorasib (LY3537982) (Eli Lilly and Company), Zipalertinib (Cullinan Oncology/Taiho Pharma), Ceralasertib (AZD6738) (AstraZeneca), TEDOPI (EP-2101; IDM 2101; OSE-2101) (OSE Immuno-therapeutics), Sigvotatug vedotin (PF08046047) (Pfizer), ANKTIVA (N-803) (ImmunityBio), Aumolertinib/Almonertinib/HS-10206 (Jiangsu Hansoh Pharmaceutical), Niraparib (GSK), Savolitinib (AstraZeneca/Hutchison MediPharma), TRODELVY (Gilead Sciences), Pyrotinib (Jiangsu HengRui Medicine), Ociperlimab (BGB-A1217) (BieGene), Volrustomig (AstraZeneca), Gotistobart (BNT316/ONC-392) (OncoC4/BioNTech), Ivonescimab (AK112/SMT112) (Akeso Biopharma/Summit Therapeutics), ZYNYZ (retifanlimab/INCMGA00012) (Incyte/Macrogenics), Divarasib (GDC-6036) (Roche/Genentech), Tiragolumab (RG6058) (Roche), Sacituzumab Tirumotecan (Merck and Kelun-Biotech), JEMPERLI (dostarlimab/TSR-042) (GSK and AnaptysBio), Zongertinib (BI-1810631) (Boehringer Ingelheim), BAY 2927088 (Bayer), Serplulimab (HLX10) (Shanghai Henlius Biotech), Rilvegostomig (AZD2936) (AstraZeneca), MK-1084 (Merck, Taiho Pharmaceutical, and Astex), Domvanalimab (Arcus Biosciences and Gilead Sciences), OPDUALAG (nivolumab and relatlimab) (Bristol-Myers Squibb), Belrestotug + JEMPERLI (iTeos Therapeutics and GSK), Firmonertinib (ArriVent BioPharma), Sunvozertinib (DZD9008) (Dizal Pharmaceutical), Cobolimab (GSK), Livmoniplimab (AbbVie), Fianlimab (REGN3767) (Regeneron Pharmaceuticals), BNT327/PM8002 (Biotheus/BioNTech), HS-20117 (Hansoh BioMedical), IO102-IO103 + Pembrolizumab (IO Biotech), Naptumomab estafenatox (NeoTX Therapeutics/Active Biotech), FF-10832 (FUJIFILM Corporation), BNT116 (BioNTechSE/Regeneron Pharmaceuticals), CAN-2409 (Candel Therapeutics), Mecbotamab Vedotin (BA3011/CAB-AXL-ADC) (BioAtla), Bemcentinib (BGB 324/BGB-3234/R-428) (BerGenBio/Rigel Pharmaceuticals), DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Lifileucel (Iovance Biotherapeutics), IBI363 (Innovent Biologics), Sotevtamab (AB-16B5) (Alethia Biotherapeutics), Avutometinib (VS6766) (Verastem Oncology), Vebreltinib (APL-101) (Apollomics), LP-300 (Lantern Pharma), JNJ-90301900 (Johnson & Johnson Innovative Medicine), AMG 193 (Amgen), Luveltamab tazevibulin (Sutro Biopharma), PRT3789 (Prelude Therapeutics), Disitamab vedotin (Seagen), PADCEV (enfortumab vedotin) (Astellas Pharma), RP1 (Replimune), TIVDAK (tisotumab vedotin) (Seagen), Zanidatamab (Jazz Pharmaceuticals), Utidelone injectable (UTD1) (Beijing Biostar Pharmaceuticals), REGN5093-M114 (Regeneron Pharmaceuticals), SLC-391 (SignalChem Lifesciences), fulzerasib (GenFleet), Davutamig (REGN5093) (Regeneron Pharmaceuticals), TAS3351 (Taiho Oncology), H002 (RedCloud Bio), JIN-A02 (J INTS BIO), FWD1509 (Forward Pharma), Sabestomig (AZD7789) (AstraZeneca), Sasanlimab (Pfizer), Selvigaltin (GB1211) (Galecto Biotech), Vepafestinib Helsinn (Healthcare/Taiho Pharmaceutical), EP0031 (A400/ KL590586) (Ellipses Pharma/Kelun-Biotech), Pamvatamig (MCLA-129) (Merus), Zidesamtinib (NVL-520) (Nuvalent), NVL-655 (Nuvalent), RMC-4630 (Revolution Medicines), REQORSA (quaratusugene ozeplasmid) (Genprex), PDC*lung01 (PDC*line Pharma), Evalstotug (BA3071) (BioAtla and BeiGene), PT-112 (Promontory Therapeutics), MRT-2359 (Monte Rosa Therapeutics), GAIA-102 (GAIA BioMedicine), Rigosertib (Traws Pharma), HMBD-001 (Hummingbird Bioscience), PLB1004 (Avistone Biotechnology), ANS03 (Avistone Biotechnology), MYTX-011 (Mythic Therapeutics), A166 (Sichuan Kelun-Biotech Bio-pharmaceutical), Atamparib (BN-2397) (Ribon Therapeutics), DELTACEL (KB-GDT-01) (Kiromic BioPharma), Carotuximab (ENV-105) (Kairos Pharma), YL202 (MediLink Therapeutics), and others. To know more about the number of competing drugs in development, visit @ TEPMETKO Market Positioning Compared to Other Drugs Key Milestones of TEPMETKO In February 2024, the FDA granted traditional approval to TEPMETKO for adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. In February 2022, the EC approved TEPMETKO as monotherapy for the treatment of adult patients with advanced NSCLC harboring alterations leading to METex14 skipping who require systemic therapy following prior treatment with immunotherapy and/or platinum-based chemotherapy. In February 2021, Merck announced that the US FDA has approved TEPMETKO following priority review for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. This indication was approved under accelerated approval based on ORR and DOR. In October 2020, TEPMETKO received ODD for treating NSCLC with MET genomic tumor aberrations In March 2020, EMD Serono (the biopharmaceutical business of Merck KGaA), announced that the MHLW approved TEPMETKO for the treatment of patients with unresectable, advanced, or recurrent NSCLC with METex14 skipping alterations. In September 2019, the US FDA granted BTD for tepotinib in patients with metastatic NSCLC harboring METex14 skipping alterations who progressed following platinum-based cancer therapy Discover how TEPMETKO is shaping the NSCLC treatment landscape @ TEPMETKO NSCLC TEPMETKO Market Dynamics TEPMETKO competes in a growing but highly specialized market where MET-targeted therapies are gaining traction due to their efficacy in addressing MET-altered tumors. The market for MET inhibitors is expanding as precision oncology advances and molecular diagnostics become more widely available, enabling better identification of patients who would benefit from targeted treatments like TEPMETKO. A key factor shaping TEPMETKO's market dynamics is competition. It directly competes with Novartis' TABRECTA (capmatinib), another MET inhibitor approved for the same indication. While TEPMETKO offers the advantage of once-daily dosing compared to TABRECTA's twice-daily regimen, both drugs have similar efficacy profiles, making physician and patient preference an important differentiator. Additionally, broader competition from next-generation MET inhibitors and combination therapies in clinical trials could impact TEPMETKO's long-term market position. Regulatory approvals and market access play a crucial role in TEPMETKO's adoption. The drug has been approved in multiple regions, including the U.S., Europe, and Japan, but reimbursement and pricing strategies vary by market. Payer policies, along with the cost-benefit analysis of MET inhibitors compared to other targeted therapies, influence prescription trends. Furthermore, real-world evidence and post-marketing studies will be critical in demonstrating TEPMETKO's sustained effectiveness and safety, which could support expanded indications and increased market penetration. Looking ahead, the MET inhibitor market is expected to grow with advances in biomarker-driven therapy, further refining patient selection. TEPMETKO's success will depend on continued clinical development, potential label expansions, and strategic partnerships to strengthen its competitive edge. As new entrants emerge, Merck KGaA's ability to differentiate TEPMETKO through combination strategies or enhanced formulations may determine its long-term sustainability in this evolving landscape. Dive deeper to get more insight into TEPMETKO's strengths & weaknesses relative to competitors @ TEPMETKO Market Drug Report Table of Contents Related Reports Non-small Cell Lung Cancer Market Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key NSCLC companies including Daiichi Sankyo, AstraZeneca, Gilead Sciences, BieGene, AbbVie, Roche, Merck, Novartis, Pfizer, Takeda Pharmaceuticals, Eli Lilly, BerGenBio, GlaxoSmithKline, Duality biologics, among others. Non-small Cell Lung Cancer Pipeline Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key non-small cell lung cancer companies, including BridgeBio Pharma, Daiichi Sankyo, EMD Serono, Merck, BridgeBio Pharma, Abbvie, Pfizer, Eli Lilly and Company BioNTech SE, Shenzhen TargetRx, Taiho Pharmaceutical, Chong Kun Dang, Bristol Myers Squibb, Innovent Biologics, Xuanzhu Biopharmaceutical, Bayer, GeneScience Pharmaceuticals, InventisBio, Apollomics, Imugene, Ono Pharmaceutical, Pierre Fabre, Jiangsu Hengrui Medicine Co., Bristol-Myers Squibb, Surface Oncology, Inhibrx, Sinocelltech, Mirati Therapeutics, REVOLUTION Medicines, Yong Shun Technology Development, Iovance Biotherapeutics, Galecto Biotech, among others. C-MET Metastatic Non-small Cell Lung Cancer Market C-MET Metastatic Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key C-MET mNSCLC companies, including Novartis, Merck, EMD Serono, AbbVie, Regeneron Pharmaceuticals, Mythic Therapeutics, Apollomics, Johnson & Johnson Innovation, Haihe Biopharma, among others. C-MET Non-small Cell Lung Cancer Pipeline C-MET Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key C-MET non-small cell lung cancer companies, including AbbVie, Janssen Research & Development, Beijing Pearl Biotechnology Limited Liability Company, Novartis, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalImmunotherapyPriority Review

04 Mar 2025

·www.pharmaceutical-technology.com

Nuvation Bio secures $250m for taletrectinib commercialisation

The financial move is set to support Nuvation Bio’s present clinical-stage pipeline development. Credit: Gorodenkoff/Shutterstock. Nuvation Bio has secured $250m in non-dilutive financing from Sagard Healthcare Partners to fully fund the commercialisation of taletrectinib in the US. The financial move will support Nuvation Bio’s present clinical-stage pipeline development. It offers potential profitability without requiring additional capital raising. The financing agreement includes a $150m royalty interest financing and an up-to-$100m senior term loan. Sagard will offer an upfront payment of $150m in cash to Nuvation Bio contingent on US Food and Drug Administration (FDA) approval of the therapy by September 2025. In exchange, Sagard will obtain tiered royalties on the therapy’s US net sales. The company will earn 5.5% of annual net sales up to $600m and 3% on sales between $600m and $1bn. Nuvation Bio will retain complete yearly US net sales exceeding $1bn. Royalty payments to Sagard will stop once they reach between 1.6 and 2 times the initial investment, depending on the date. Sagard has also committed to an up-to-$100m five-year, senior secured term loan. The first tranche of $50m will be available upon FDA approval of the therapy, and the second tranche is accessible until 30 June 2026, subject to Nuvation Bio’s achievement of the first US commercial sale of taletrectinib. Sidley Austin served as legal advisor to Sagard. TD Cowen acted as the financial advisor, while Cooley provided legal counsel to Nuvation Bio. Nuvation Bio CEO, president and founder David Hung stated: “With these financings, we are well positioned to launch taletrectinib and drive continued development of our clinical-stage pipeline — all without the need for additional fundraising. “ We are thrilled to have support from Sagard and appreciate their shared confidence in taletrectinib and Nuvation Bio as we continue toward our goal of improving outcomes for patients with cancer.” In January 2022, Nuvation Bio received FDA clearance for its investigational new drug application for NUV-868, targeting advanced solid tumours.

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100 Deals associated with Taletrectinib

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

Developing

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

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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)	xyxspxzptm(jvesfykjcy): 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	gkijkmctdp(jtrrjonlnr) = ehirnlxmmi rtvjfjvoeb (jjfuzgusue ) View more	Positive	14 Sep 2024
				Taletrectinib Taletrectinib 600 mg QD (1 prior ROS1 TKI)	gkijkmctdp(jtrrjonlnr) = luwgwrhkoq rtvjfjvoeb (jjfuzgusue, 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)	unmehcbscj(rhfotwobqb) = jhwhywoumz xrpsucsdby (jtlxboxybs ) View more	Positive	01 Jun 2024
				Taletrectinib (crizotinib pretreated)	unmehcbscj(rhfotwobqb) = slhvfpztee xrpsucsdby (jtlxboxybs ) View more
NCT04395677 (TRUST-I, Pubmed \| J Clin Oncol)	Phase 2	Non-Small Cell Lung Cancer ROS1+	173	Taletrectinib	wtixvmevux(wfyjajsyga) = bfkeqguhsc xvqxcdcljf (sjmarcjzzr ) View more	Positive	01 Jun 2024
				Crizotinib	wtixvmevux(wfyjajsyga) = ldpynaoezo xvqxcdcljf (sjmarcjzzr ) View more
NCT04395677 (TRUST-I, ASCO2024 \| NEWS) Manual	Phase 2	Reactive oxygen species 1 positive non-small cell lung cancer ROS1 G2032R	173	Taletrectinib	nteexzhavb(ngorvdahax) = kgljipgkyn maokmbofzp (ebpicouexu, 83 - 95) View more	Positive	24 May 2024
				Chemotherapy	nteexzhavb(ngorvdahax) = dprkavcsyj maokmbofzp (ebpicouexu, 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))	omtnpxiihb(cvopvgwyvo) = hmnihajyka oaiivxptbq (csulztizzw ) View more	Positive	23 Oct 2023
				Taletrectinib (NSCLC: 1 prior ROS1 TKI, ≤1 line of CT)	omtnpxiihb(cvopvgwyvo) = ihnjlbnfpx oaiivxptbq (csulztizzw ) 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)	rixwomedtv(ixdwfgnces) = xvbqoglqlx usgagcskvh (pwrozvniok, 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)	ofyorihznz(ycfgldovtd) = eslczoilan ixszcbyhca (qhdgwefyuk, 83.1 - 99.4) View more	Positive	02 Jun 2022
				Taletrectinib 600mg (crizotinib-pretreated cohort)	ofyorihznz(ycfgldovtd) = fjznhfybgj ixszcbyhca (qhdgwefyuk, 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	wlbmtxbltf(tlubdtdgft) = piywkofkiy ikmfosksmy (xqnvnstbjy, 72% - 100%) View more	Positive	28 May 2021
				Taletrectinib 600 mg QD	gnppamwlrz(mdvxkvxvjc) = qngzsprqrd ekvtrysgwh (hxcqsedcuy ) View more
NCT02279433 (Pubmed \| Clin Cancer Res) Manual	Phase 1	HR-positive/HER2-low Solid Tumors	46	Taletrectinib	qpqartrsoe(jinznkpzus) = grade 3 transaminases increase occurred in two patients (1,200-mg once-daily dose) kvlixmmxhd (ehmqixrtzf ) View more	Positive	15 Sep 2020

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