Augtyro (repotrectinib) / ZAI Lab, BMS - LARVOL DELTA

NCCN has published NEW NCCN Guidelines in the NCCN Guidelines Navigator. This interactive digital tool can be used to navigate the current version of the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines) for Uterine Neoplasms, Version 3.2025. (NCCN)

NCCN guideline • Microsatellite Instability • Uterine Cancer

Reporos trial-GFPC 04-2023: open-label phase II efficacy study of repotrectinib in frail patients with ROS1-rearranged metastatic NSCLC (ESMO 2025) - No abstract available

Clinical • Metastases • P2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ROS1

Repotrectinib in Adult and Pediatric Patients with NTRK+ Advanced Solid Tumors: Updated Results From the TRIDENT-1 and CARE Trials (ESMO 2025) - No abstract available

Clinical • Metastases • Oncology • Solid Tumor • NTRK

Taletrectinib (Ibtrozi) - another kinase inhibitor for non-small cell lung cancer (NSCLC). (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Phase II Study of Repotrectinib in ROS1-Positive Non-Small Cell Lung Cancer Patients With Active Brain Metastasis - REPOSE (IASLC-WCLC 2025) - "Abstract is embargoed at this time."

Clinical • P2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ROS1

Population-Adjusted Indirect Comparisons of Repotrectinib and Taletrectinib in ROS1+ aNSCLC (IASLC-WCLC 2025) - "Abstract is embargoed at this time."

Clinical • Non Small Cell Lung Cancer • Solid Tumor • ROS1

Repotrectinib in Patients With ROS1 Fusion-Positive (ROS1+) NSCLC: Long-Term Follow-Up From the Phase 1/2 TRIDENT-1 Trial (IASLC-WCLC 2025) - "Abstract is embargoed at this time."

Clinical • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • ROS1

Repotrectinib in ROS1 Fusion-Positive Non- Small-Cell Lung Cancer: A Systematic Review and Meta-Analysis (ERS 2025) - No abstract available

Retrospective data • Review • Lung Cancer • Oncology • Solid Tumor • ROS1

ROS1 fusion-positive non-small cell lung cancer-repotrectinib as a new treatment option. (PubMed, Transl Cancer Res) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ROS1

Discovery of imidazo[1,2-b]pyridazine derivatives as potent TRK inhibitors for overcoming multiple resistant mutants. (PubMed, Bioorg Chem) - "Tropomyosin receptor kinases (TRKs), the superfamily of transmembrane receptor tyrosine kinases, have recently attracted extensive attention as promising cancer therapeutic targets since the approval of Larotrectinib, Entrectinib and Repotrectinib by FDA. In addition, compound 15m displayed good oral bioavailability (F = 55.26 %). Collectively, compound 15m is a promising lead compound as a TRK inhibitor and deserves further structural optimization to address clinical refractory acquired resistances."

Journal • Oncology

PHARMACEUTICAL BENEFITS ADVISORY COMMITTEE (PBAC) MEETING OUTCOMES MAY 2025 PBAC MEETING: Augtyro for NSCLC (Pharmaceutical Benefits Scheme (PBS)) - "...The PBAC recommended PBS listing at an equivalent cost per day based on the steady state dosing of entrectinib and repotrectinib, with the price of the repotrectinib dose reduction pack to be derived on a weighted dose approach to maintain an equivalent cost per day to the steady state pack..."

Reimbursement • Lung Cancer • Non Small Cell Lung Cancer • Oncology

Onco360 Has Been Selected as a National Specialty Pharmacy for Augtyro (repotrectinib) (The Manila Times) - "Onco360...has added Augtyro (repotrectinib) manufactured by Bristol Myers Squibb to its comprehensive list of limited distribution therapies."

Commercial • Non Small Cell Lung Cancer • Solid Tumor

Augtyro: Newly added patent in Orange Book (Orange Book) - Expiry on Jul 20, 2036

Patent • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic Cancer

Recent advances in tropomysosin receptor kinase (TRK) inhibitors: a 2023-2024 patent landscape review. (PubMed, Expert Opin Ther Pat) - "TRK inhibitors like larotrectinib and entrectinib marked a paradigm shift - prioritizing molecular alterations over the tumor's anatomical location...Combination therapies with TRK inhibitors are emerging as a key strategy to enhance efficacy and overcome resistance. The FDA's recent approval of repotrectinib underscores progress in the TRK inhibitor landscape, while highlighting the continued need for innovation."

Journal • Review • Oncology • NTRK

Creating Repotrectinib Resistance in a Ba/F3 SLC34A2-ROS1 NSCLC cell line (EACR 2025) - "We generated three Ba/F3 SLC34A2-ROS1 repotrectinib resistant cell lines. A short term repotrectinib withdrawal makes the resistant cells more sensitive to repotrectinib. Mechanisms underlying the observed resistance such as mutations in the tyrosine kinase domain or in genes affecting alternative signaling pathways are currently being examined."

Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ROS1 • SLC34A2

Assessment of two new ROS1+ NSCLC patient-derived cell lines as in vitro models for TKI resistance studies (EACR 2025) - "The IC50 values of unmutated ROS1+ Ba/F3 cells for crizotinib, entrectinib, lorlatinib, repotrectinib and zidesamtinib were 31.4; 44.6; 14.3; 14.9 and 29.9 nM, respectively...Interestingly, these cells were resistant to lorlatinib, while the patient is – after being treated with lorlatinib+cis-platinum+pemetrexed, now currently successfully treated with lorlatinib mono-therapy... In this study we showed that PC1 cells generated from a crizotinib-resistant patient were resistant to all ROS1 inhibitors tested. The G2032R mutated PC2 cells generated from a crizotinib and lorlatinib resistant patient were sensitive to repotrectinib, but not to zidesamtinib. This PC2 cell line can be used to assess off-target resistance mechanism to zidesamtinib."

Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Respiratory Diseases • Solid Tumor • ARID1A • CD74 • PIK3CA • PIK3CG • ROS1

The interplay between mechanisms of resistance and therapeutic targets: identifying novel treatments for drug-resistant BRAFV600E pediatric high-grade glioma (EACR 2025) - "Similarly, dabrafenib (BRAFi)-treated animals orthotopically administered with the vemurafenib-resistant culture had significantly reduced survival compared to treated animals administered with the matched parental cells (65 days vs 79 days)...Repotrectinib (NTRK2/SRCi) and dacomitinib (EGFRi) were found to display potent synergistic activity when used in combination with vemurafenib (BRAFi) against both vemurafenib-resistant BRAFV600E pHGG cells and matched parental cells in vitro... This study has demonstrated that analyzing tumor mechanisms is a powerful tool for identifying effective therapies in treatment-refractory tumors. Using an omics-based approach in BRAFV600E pHGG, we have identified novel drivers of drug resistance, key therapeutic targets and several promising therapeutic options."

Clinical • Brain Cancer • Glioma • High Grade Glioma • Oncology • Pediatrics • Solid Tumor • EGFR • NTRK2

Durable Response in NTRK Fusion-Positive Advanced Salivary Gland Tumor: A Case Report. (PubMed, Case Rep Oncol) - "Recent studies have shown that TRK inhibitors, such as entrectinib, larotrectinib and repotrectinib, are effective in treating solid tumors harboring NTRK gene fusions. To our knowledge, this is the first reported case in Bolivia of a salivary gland tumor with an NTRK fusion identified through molecular profiling, followed by successful treatment with compassionate use of entrectinib. This case not only demonstrates the therapeutic benefits and safety of NTRK inhibitors but also underscores the importance of personalized therapy guided by molecular profiling in oncology."

Journal • Oncology • Salivary Gland Cancer • Solid Tumor • NTRK

Repotrectinib for ROS1 positive non-small cell lung cancer, pre-treated with crizotinib (PubMed, Bull Cancer) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ROS1

Repotrectinib in advanced cancers with NTRK fusion after progression or not on a first TRK inhibitor (PubMed, Bull Cancer) - No abstract available

Journal • Oncology • NTRK

KFDA approves BMS cancer drug lepotrectinib for rare lung cancer treatments (Chosun Biz) - "The Ministry of Food and Drug Safety announced on the 5th that it has granted approval for the rare drug 'Octairo Capsule (ingredient name repotrectinib).' The importer is Korea BMS Pharmaceutical."

Approval • Non Small Cell Lung Cancer

Osimertinib plus repotrectinib phase I trial in TKI-resistant non-small cell lung cancer (NSCLC) with EGFR mutations. (ASCO 2025) - P1 | "The findings prompted us to carry out the current study with osimertinib plus TPX-0005, which inhibit Src/FAK/JAK2, in addition to ALK, ROS1 and NTRKs. In Part Ia osimertinib + repotrectinib showed impressive intracranial ORR with a manageable safety profile. Part Ib with repotrectinib 160 mg BID plus osimertinib 80 mg is ongoing. Updated results will be presented."

P1 data • Anemia • Fatigue • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • CDK4 • EGFR • FAT1 • FGFR3 • MET • MYC • PIK3CA • ROS1 • STAT3 • TP53 • YAP1

Biomarker testing in metastatic colorectal cancer (mCRC): 2015-2024 trends in the United States (US) community oncology setting. (ASCO 2025) - "In 2020, following the approval of tucatinib, HER2 testing rates increased from 32%-66% prior to 2019 to 89%-93% after 2020. BRAF testing rates also increased to 90%-96% after 2017, following the approval of encorafenib plus cetuximab combination therapy for BRAF-mutated mCRC in 2018. NTRK testing rates (21%-42%) showed improvement over the study period, with the highest proportion of patients tested in 2024 corresponding to the accelerated approval of repotrectinib for in the same year. Similarly, RET testing (25%-89%) peaked in 2023 following breakthrough therapy designation for selpercatinib in late 2022... As new targeted therapies have emerged in recent years, biomarker testing rates for mCRC have rapidly increased in the community oncology setting. NTRK or RET rearrangements are infrequent in advanced CRC, with lower testing rates for these genes within the study period. However, as this study leveraged structured data only, actual rates of testing may be even..."

Biomarker • Metastases • Colorectal Cancer • Oncology • Solid Tumor • BRAF • HER-2 • KRAS • NRAS • NTRK

Progression-Free Survival and Objective Response Rates As Surrogate Endpoints for Overall Survival Among Patients With ROS1+ Locally Advanced or Metastatic Non-Small Cell Lung Cancer Receiving ROS1 Tyrosine Kinase Inhibitors (ISPOR 2025) - " Twelve cohorts from non-randomized clinical trials involving treatment with crizotinib, entrectinib, lorlatinib, brigatinib or ceritinib were identified; repotrectinib cohorts were excluded. The current analysis demonstrated a strong association between OS and PFS among TKI-treated patients with ROS1+ aNSCLC, lending support to previous real world evidence evaluating surrogacy of PFS. However, OS and ORR demonstrated a weak association with substantial uncertainty. The lack of head-to-head evidence precluded assessment of the correlation between treatment effects."

Clinical • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ROS1

Discovery of novel diarylurea derivatives as potent type II TRK inhibitors for combating multiple acquired resistant mutants. (PubMed, Bioorg Chem) - "Tropomyosin receptor kinases (TRKs), a superfamily of transmembrane receptor tyrosine kinases, have recently attracted extensive attention as promising cancer therapeutic targets since the FDA approval of Larotrectinib and Entrectinib. It also showed superior antiproliferative activities against both BaF3-LMNA-TRKAG595R and BaF3-LMNA-TRKAG667C cell lines (IC50 = 23.76 nM and 0.33 nM, respectively), outperforming Repotrectinib (IC50 = 28.14 nM and 25.69 nM, respectively). Collectively, compound 18d can be used as a promising lead candidate for further optimization in the development of therapies targeting drug-resistant TRK mutants."

Journal • Oncology • LMNA