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    DRUG CLASS:

    TrkA receptor antagonist

    Related drugs:
    2ms
    Application of newly developed and validated UPLC-MS/MS method for pharmacokinetic study of ROS1/NTRK inhibitor taletrectinib in beagle dog plasma. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci)
    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).
    PK/PD data • Journal
    |
    NTRK (Neurotrophic receptor tyrosine kinase)
    |
    taletrectinib (AB-106)
    3ms
    A Phase III Study Comparing Taletrectinib With Standard Therapy in ROS1 Positive Locally Advanced or Metastatic Non-small Cell Lung Cancer Patients (clinicaltrials.gov)
    P3, N=138, Not yet recruiting, AnHeart Therapeutics Inc.
    New P3 trial • Metastases
    |
    Xalkori (crizotinib) • taletrectinib (AB-106)
    5ms
    Taletrectinib: TRUST in the Continued Evolution of Treatments for ROS1 Fusion-Positive Lung Cancer. (PubMed, J Clin Oncol)
    No abstract available
    Journal
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    taletrectinib (AB-106)
    6ms
    Efficacy and Safety of Taletrectinib in Chinese Patients With ROS1+ Non-Small Cell Lung Cancer: The Phase II TRUST-I Study. (PubMed, J Clin Oncol)
    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.
    P2 data • Journal
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    Xalkori (crizotinib) • taletrectinib (AB-106)
    6ms
    Selective TrkA Inhibitor VMD-928 to Treat TrkA Overexpression Driven Solid Tumors or Lymphoma (clinicaltrials.gov)
    P1, N=74, Recruiting, VM Oncology, LLC | Trial completion date: Dec 2025 --> Jun 2026 | Trial primary completion date: Jun 2025 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1)
    |
    VMD-928
    7ms
    Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC) (clinicaltrials.gov)
    P2, N=61, Not yet recruiting, Megan Kruse, MD | Initiation date: Apr 2024 --> Oct 2024
    Trial initiation date • Metastases
    |
    Xalkori (crizotinib) • taletrectinib (AB-106)
    9ms
    TRUST-II: Taletrectinib Phase 2 Global Study in ROS1 Positive NSCLC (clinicaltrials.gov)
    P2, N=224, Recruiting, AnHeart Therapeutics Inc. | N=154 --> 224
    Enrollment change • Metastases
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ROS1 fusion
    |
    taletrectinib (AB-106)
    10ms
    Taletrectinib in Previously Treated Metastatic CDH1-mutated Invasive Lobular Cancer (ILC) (clinicaltrials.gov)
    P2, N=61, Not yet recruiting, Megan Kruse, MD
    New P2 trial • Metastases
    |
    Xalkori (crizotinib) • taletrectinib (AB-106)
    10ms
    Taletrectinib for the treatment of ROS-1 positive non-small cell lung cancer: a drug evaluation of phase I and II data. (PubMed, Expert Opin Investig Drugs)
    While crizotinib and entrectinib have been approved to treat ROS1 fusion-positive (ROS1+) non-small-cell lung cancer (NSCLC), unmet needs remain. Taltrectinib has the potential to improve PFS based on its greater potency against ROS1+ tumors and high CNS penetration. By selectively inhibiting ROS1 wild-type and its resistant mutations over TRKB, taltrectinib has a better safety profile with minimal CNS-related AEs compared to other ROS1+ inhibitors.
    P1 data • Review • Journal
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2)
    |
    ROS1 fusion • ROS1 positive • ROS1 wild-type
    |
    Xalkori (crizotinib) • Rozlytrek (entrectinib) • taletrectinib (AB-106)
    11ms
    Selective TrkA Inhibitor VMD-928 to Treat TrkA Overexpression Driven Solid Tumors or Lymphoma (clinicaltrials.gov)
    P1, N=74, Recruiting, VM Oncology, LLC | Trial completion date: Jun 2025 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Jun 2025
    Trial completion date • Trial primary completion date
    |
    NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1)
    |
    NTRK1 fusion • NTRK1 mutation • NTRK expression
    |
    VMD-928
    11ms
    AnHeart Therapeutics and Foundation Medicine Announce Collaboration to Develop Tissue-Based and Liquid-Based Companion Diagnostics for Taletrectinib, a ROS1 Inhibitor (Businesswire)
    "AnHeart Therapeutics...and Foundation Medicine, Inc., today announced the companies have entered a strategic collaboration for the development and regulatory approval of Foundation Medicine’s tissue-based and liquid-based comprehensive genomic profiling tests, FoundationOne®CDx and FoundationOne®Liquid CDx, as companion diagnostics for AnHeart’s investigational next-generation ROS1 inhibitor, taletrectinib, in the United States....Taletrectinib is a potential best-in-class ROS1 inhibitor being evaluated for the treatment of patients with advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC), an underserved group of lung cancer patients in need of new options."
    Licensing / partnership
    |
    FoundationOne® CDx • FoundationOne® Liquid CDx
    |
    taletrectinib (AB-106)
    1year
    TRUST: A Study of AB-106 in Subjects With Advanced NSCLC Harboring ROS1 Fusion Gene (clinicaltrials.gov)
    P2, N=173, Active, not recruiting, AnHeart Therapeutics Inc. | Recruiting --> Active, not recruiting | N=106 --> 173
    Enrollment closed • Enrollment change • Metastases
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ROS1 fusion
    |
    taletrectinib (AB-106)
    1year
    Comprehensive analysis of cuproptosis genes and cuproptosis-related genes as prognosis factors in esophageal squamous cell carcinoma. (PubMed, Genomics)
    The results also showed that milciclib might inhibit the proliferation and migration of KYSE150 and KYSE510 cells by targeting CDKN2A. In conclusion, the abovementioned CUGs and CRGs play a crucial role in tumorigenesis and cancer progression in ESCC, indicating their potential as therapeutic targets.
    Journal
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • BTLA (B And T Lymphocyte Associated) • DLAT (Dihydrolipoamide S-Acetyltransferase) • MELTF (Melanotransferrin) • PRRX1 (Paired Related Homeobox 1) • FDX1 (Ferredoxin 1) • LIAS (Lipoic Acid Synthetase) • LIPT1 (Lipoyltransferase 1) • PDHA1 (Pyruvate Dehydrogenase E1 Subunit Alpha 1)
    |
    milciclib (TZLS-201)
    over1year
    Efficacy and safety of taletrectinib in patients (Pts) with ROS1+ non-small cell lung cancer (NSCLC): Interim analysis of global TRUST-II study (ESMO 2023)
    No treatment-related AE (TRAE) led to discontinuation or death; 24% of pts had a TRAE leading to dose reduction. Conclusions In this ongoing global pivotal phase 2 study, taletrectinib demonstrated robust and consistent clinical activity with TRUST-I, including high response rates and a tolerable safety profile in both TKI-naive and TKI-pretreated pts with ROS1+ NSCLC.
    Clinical
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2)
    |
    ROS1 G2032R
    |
    taletrectinib (AB-106)
    over1year
    Selective TrkA Inhibitor VMD-928 to Treat TrkA Overexpression Driven Solid Tumors or Lymphoma (clinicaltrials.gov)
    P1, N=74, Recruiting, VM Oncology, LLC | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1)
    |
    NTRK1 fusion • NTRK1 mutation • NTRK expression
    |
    VMD-928
    over1year
    TRUST-II: a global phase II study of taletrectinib in ROS1-positive non-small-cell lung cancer and other solid tumors. (PubMed, Future Oncol)
    Crizotinib and entrectinib have been approved to treat ROS1 fusion-positive (ROS1) non-small-cell lung cancer. Secondary end points include duration of response, progression-free survival, overall survival and safety. This trial is enrolling patients in North America, Europe and Asia.
    P2 data • Review • Journal
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ROS1 fusion • ROS1 positive
    |
    Xalkori (crizotinib) • Rozlytrek (entrectinib) • taletrectinib (AB-106)
    over1year
    REGISTRI: Single Agent Regorafenib in First-line for Metastatic/Unresectable KIT/PDGFR Wild Type GIST (clinicaltrials.gov)
    P2, N=15, Completed, Grupo Espanol de Investigacion en Sarcomas | Recruiting --> Completed | N=39 --> 15
    Trial completion • Enrollment change • Metastases
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    KIT mutation • KIT exon 11 mutation • KIT exon 13 mutation • KIT exon 17 mutation • KIT wild-type • PDGFR wild-type
    |
    Stivarga (regorafenib)
    over1year
    STREAM: Regorafenib Monotherapy as Second-line Treatment of Patients With RAS-mutant Advanced Colorectal Cancer (clinicaltrials.gov)
    P2, N=46, Active, not recruiting, National Cancer Institute, Naples | Trial completion date: Nov 2022 --> Nov 2024 | Trial primary completion date: Nov 2021 --> Nov 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    RAS (Rat Sarcoma Virus)
    |
    RAS mutation
    |
    Stivarga (regorafenib)
    over1year
    Regorafenib and PD-1 Antibody in Combination With Radiotherapy for pMMR/MSS Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=28, Recruiting, Sun Yat-sen University | Unknown status --> Recruiting | N=43 --> 28 | Trial completion date: Jul 2020 --> Jul 2023 | Trial primary completion date: Jul 2020 --> Feb 2023
    Enrollment open • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS wild-type • RAS wild-type
    |
    Stivarga (regorafenib)
    over1year
    An Exploration of Trifluridine/Tipiracil Monotherapy and in Combination With Bevacizumab or Immune Checkpoint Inhibitors for Patients With Metastatic Colorectal Cancer: A Real-World Study. (PubMed, Clin Colorectal Cancer)
    In real-world clinical setting, TAS-102 showed consistent clinical efficacy and manageable safety with previous prospective clinical studies. Compared with monotherapy and TAS-102 plus ICIs, TAS-102 plus bevacizumab demonstrated better clinical efficacy for metastatic colorectal cancer.
    Journal • Combination therapy • Checkpoint inhibition • Real-world evidence • Real-world • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Avastin (bevacizumab) • Stivarga (regorafenib) • Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil)
    over1year
    Circulating Tumor DNA Dynamics and Treatment Outcome of Regorafenib in Metastatic Colorectal Cancer. (PubMed, Cancer Res Treat)
    VAF of the majority of the ctDNA mutations increased at the time of disease progression, and VAF of BRAF increased markedly. Reduction in ctDNA burden as estimated by sum (VAF) could be used to predict treatment outcome of regorafenib.
    Journal • Circulating tumor DNA • Metastases
    |
    BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • TCF7L2 (Transcription Factor 7 Like 2)
    |
    TP53 mutation
    |
    Stivarga (regorafenib)
    over1year
    Is neutrophil-to-lymphocyte ratio and C-reactive protein the prognostic role in metastatic colorectal cancer using regorafenib? (PubMed, J Gastrointest Oncol)
    No abstract available
    Journal • Metastases
    |
    CRP (C-reactive protein)
    |
    Stivarga (regorafenib)
    over1year
    Using a combination of fruquintinib, raltitrexed, and S-1 as a third-line treatment for metastatic colorectal cancer with co-existence of Hodgkin lymphoma: a case report. (PubMed, J Gastrointest Oncol)
    Fruquintinib, regorafenib, trifluridine/tipiracil (TAS-102), panitumumab and cetuximab combined with single-agent chemotherapy regimens are currently recommended as third-line therapies for patients exhibiting disease progression...The mFOLFOX6 regimen was administered...Liver metastases (intestinal-type adenocarcinoma) were detected in November 2018, and second-line therapy with the FOLFIRI regimen was initiated in January 2019...Third-line therapy with fruquintinib, raltitrexed, and S-1 achieved a PR that permitted surgical resection and enabled a relatively long progression-free survival. The findings suggest that the three agents regimen might be clinically effective as late-line therapy for mCRC.
    Clinical • Journal • Metastases
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    PIK3CA mutation • RAS wild-type
    |
    Erbitux (cetuximab) • 5-fluorouracil • Vectibix (panitumumab) • Stivarga (regorafenib) • oxaliplatin • irinotecan • Fruzaqla (fruquintinib) • Lonsurf (trifluridine/tipiracil) • leucovorin calcium • Teysuno (gimeracil/oteracil/tegafur) • Tomudex (raltitrexed)
    over1year
    A Real-World Comparison of Regorafenib and Trifluridine/Tipiracil in Refractory Metastatic Colorectal Cancer in the United States. (PubMed, J Natl Compr Canc Netw)
    This analysis of real-world data found that OS was similar for patients with mCRC who were treated with TAS-102 compared with regorafenib. Median OS with both agents in a real-world setting was similar to that shown in the clinical trials that led to their approvals. A prospective trial comparing TAS-102 and regorafenib would unlikely change current management of patients with refractory mCRC.
    Journal • Real-world evidence • Real-world • Metastases
    |
    MSI (Microsatellite instability)
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    over1year
    Adeno-associated virus-mediated knockdown demonstrates the major role of hepatic Bcrp in the overall disposition of the active metabolite of the tyrosine kinase inhibitor regorafenib in mice. (PubMed, Drug Metab Pharmacokinet)
    AAV-shBcrp-treated mice showed higher M - 5 concentration in plasma and liver, but lower biliary excretion than the control mice, indicating the fundamental role of hepatic Bcrp in M - 5 disposition. This is the first application of AAV-knockdown strategy to clarify the pharmacokinetic role of xenobiotic efflux transporters in the liver.
    Preclinical • Journal
    |
    CRP (C-reactive protein)
    |
    Stivarga (regorafenib)
    over1year
    ReDOS: Lower or Standard Dose Regorafenib in Treating Patients With Refractory Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=123, Completed, Academic and Community Cancer Research United | Trial completion date: Jun 2025 --> Mar 2023 | Active, not recruiting --> Completed
    Trial completion • Trial completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS wild-type • RAS wild-type
    |
    Stivarga (regorafenib)
    over1year
    Efficacy of third-line anti-EGFR-based treatment versus regorafenib or trifluridine/tipiracil according to primary tumor site in RAS/BRAF wild-type metastatic colorectal cancer patients. (PubMed, Front Oncol)
    Our results demonstrated a different benefit from third-line anti-EGFR-based therapy according to primary tumor site, confirming the role of L-sided tumor in predicting benefit from third-line anti-EGFR vs R/T. At the same time, no difference was observed in R-sided tumor.
    Journal • Metastases
    |
    BRAF (B-raf proto-oncogene) • RAS (Rat Sarcoma Virus)
    |
    BRAF wild-type
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    over1year
    EGFR and Lyn inhibition augments regorafenib induced cell death in sorafenib resistant 3D tumor spheroid model. (PubMed, Cell Signal)
    Patients with unresectable HCC receive systemic therapies, traditionally sorafenib or lenvatinib as first line therapy. Importantly, combined inhibition of EGFR and Lyn kinase in sorafenib resistant tumor spheroids are effective in inducing cell death. Our model proved to be an affordable and useful model to mimic drug resistant tumor microenvironment in HCC and provided novel insights into candidates for new combinational therapies.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • LYN (LYN Proto-Oncogene Src Family Tyrosine Kinase) • CD24 (CD24 Molecule)
    |
    sorafenib • Lenvima (lenvatinib) • Stivarga (regorafenib)
    over1year
    Use of Novel m6A Regulator-mediated Methylation Modification Patterns in Distinct Tumor Microenvironment Profiles to Identify and Predict Glioma Prognosis and Progression, T-cell Dysfunction, and Clinical Response to ICI Immunotherapy. (PubMed, Curr Pharm Des)
    Glioma m6A clusters and gene signatures have distinctive TME features. The m6A gene signature may guide prognostic assessments and promote the use of effective strategies.
    Journal • Tumor mutational burden • IO biomarker
    |
    TMB (Tumor Mutational Burden)
    |
    Avastin (bevacizumab) • Stivarga (regorafenib)
    over1year
    Efficacy and Safety of Regorafenib Plus Immune Checkpoint Inhibitors with or Without TACE as a Second-Line Treatment for Advanced Hepatocellular Carcinoma: A Propensity Score Matching Analysis. (PubMed, J Hepatocell Carcinoma)
    The difference in the incidence of TRAEs between the two groups was not statistically significant (P> 0.05). Compared to regorafenib plus ICIs, regorafenib plus ICIs with TACE was tolerated and improved survival as the second-line treatment for patients with advanced HCC.
    Journal • Checkpoint inhibition • Metastases
    |
    AFP (Alpha-fetoprotein)
    |
    Stivarga (regorafenib)
    over1year
    Baseline Cytokine Profile Identifies a Favorable Outcome in a Subgroup of Colorectal Cancer Patients Treated with Regorafenib. (PubMed, Vaccines (Basel))
    This report suggests that the analysis of multiple cytokines might identify a cytokine signature related to a patient's outcome that is able to recognize patients who will benefit from treatment. If confirmed, future studies, also based on different drugs, using this approach and including larger patient populations, might identify a signature allowing the a priori identification of patients to be treated.
    Journal
    |
    IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • IL10 (Interleukin 10) • CCL2 (Chemokine (C-C motif) ligand 2) • TGFB1 (Transforming Growth Factor Beta 1) • IL13 (Interleukin 13) • IL21 (Interleukin 21)
    |
    Stivarga (regorafenib)
    over1year
    Insights into the medical management of gastrointestinal stromal tumours: lessons learnt from a dedicated gastrointestinal stromal tumour clinic in North India. (PubMed, Ecancermedicalscience)
    The most common change was the use of sunitinib and regorafenib in patients with SDH-deficient GIST. The mutation testing rates at primary care centres continue to be low. Despite the hurdles, a large percentage of our patients underwent molecular testing, aiding in therapeutic decision-making.
    Journal • Stroma
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    sunitinib • Stivarga (regorafenib)
    almost2years
    Emerging Data on the Safety and Efficacy of Ripretinib for the Treatment of Gastrointestinal Stromal Tumors. (PubMed, Clin Exp Gastroenterol)
    Sunitinib and regorafenib are approved in the second- and third-line setting, respectively, with activity against certain secondary mutations with comparatively much lower response rates and survival increment compared to imatinib. Although the efficacy of ripretinib in this unselected patient population was not significantly different from that of sunitinib, the tolerability profile was better. This review article aims to review the efficacy and tolerability profile of ripretinib, together with its role in the setting of unresectable or metastatic GIST.
    Clinical • Review • Journal • Stroma
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    imatinib • sunitinib • Stivarga (regorafenib) • Qinlock (ripretinib)
    almost2years
    Leronlimab in Combination With Regorafenib in Patients With CCR5+, Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=0, Withdrawn, CytoDyn, Inc.
    New P2 trial • Combination therapy • Metastases
    |
    RAS wild-type
    |
    Stivarga (regorafenib) • Vyrologix (leronlimab)
    almost2years
    Survival improvement for patients with metastatic colorectal cancer over twenty years. (PubMed, NPJ Precis Oncol)
    Notably, survival improved for patients with BRAF mutant as well as microsatellite unstable (MSI-H) tumors. Multivariate regression analysis identified surgical resection of liver metastasis (HR = 0.26, 95% CI, 0.19-0.37), use of immunotherapy (HR = 0.44, 95% CI, 0.29-0.67) and use of third line chemotherapy (regorafenib or trifluridine/tipiracil, HR = 0.74, 95% CI, 0.58-0.95), but not year of diagnosis (HR = 0.99, 95% CI, 0.98-1), as associated with better survival, suggesting that increased use of these therapies are the drivers of the observed improvement in survival.
    Journal • MSi-H Biomarker • IO biomarker • Metastases
    |
    BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability)
    |
    MSI-H/dMMR • BRAF mutation
    |
    Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    almost2years
    Regorafenib is suitable for advanced colorectal cancer patients who have previously received trifluridine/tipiracil plus bevacizumab. (PubMed, Sci Rep)
    The major grade 3 and4 toxicities were proteinurea (29%), hypertension (26%), hand-foot syndrome(15%), and platelet decrease (6%). Regorafenib after TFTD plus bevacizumab showed efficacy similar to that of the previous study, and no new adverse events were observed.
    Journal • Metastases
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF V600E • BRAF V600 • RAS mutation
    |
    Avastin (bevacizumab) • Stivarga (regorafenib) • Lonsurf (trifluridine/tipiracil)
    almost2years
    Clinical activity of regorafenib in elderly patients with recurrent glioblastoma. (PubMed, Mol Clin Oncol)
    MGMT methylation appeared to influence OS. To the best of our knowledge, this was the first report of regorafenib activity in older patients and, while the results were statistically significant, these should be confirmed in further studies.
    Journal
    |
    MGMT (6-O-methylguanine-DNA methyltransferase)
    |
    Stivarga (regorafenib)
    almost2years
    Updated Efficacy and Safety of Taletrectinib in Patients (pts) with ROS1+ Non-Small Cell Lung Cancer (NSCLC) (ELCC 2023)
    CRZ, crizotinib; DCR, disease control rate; NE, not evaluable; ORR, overall response rate; PFS, progression-free survival; TKI, tyrosine kinase inhibitor. Conclusions With additional follow-up, taletrectinib continued to demonstrate meaningful efficacy outcomes including high response rates, prolonged PFS, robust intracranial activity, activity against G2032R, and tolerable safety with low incidence of neurological AEs.
    Clinical
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2)
    |
    ROS1 G2032R
    |
    Xalkori (crizotinib) • taletrectinib (AB-106)
    almost2years
    REPROGRAM-01: Regorafenib in Combination With Metronomic Chemotherapies, and Low-dose Aspirin in Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=49, Active, not recruiting, Centre Hospitalier Universitaire de Besancon | Trial primary completion date: Jan 2023 --> Jul 2023
    Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    RAS wild-type • NRAS wild-type
    |
    capecitabine • cyclophosphamide • Stivarga (regorafenib) • aspirin
    almost2years
    MegaMOST: A Study Evaluating the Activity of Anti-cancer Treatments Targeting Tumor Molecular Alterations/Characteristics in Advanced / Metastatic Tumors. (clinicaltrials.gov)
    P2, N=425, Recruiting, Centre Leon Berard | Trial completion date: Nov 2024 --> Nov 2026 | Trial primary completion date: Feb 2024 --> Feb 2026
    Trial completion date • Trial primary completion date • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • FLT3 (Fms-related tyrosine kinase 3) • NRAS (Neuroblastoma RAS viral oncogene homolog) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • HRAS (Harvey rat sarcoma viral oncogene homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • NF1 (Neurofibromin 1) • AXL (AXL Receptor Tyrosine Kinase) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11) • SMAD4 (SMAD family member 4) • RAF1 (Raf-1 Proto-Oncogene Serine/Threonine Kinase) • FLT1 (Fms-related tyrosine kinase 1) • CDK6 (Cyclin-dependent kinase 6) • CCND3 (Cyclin D3) • TYRO3 (TYRO3 Protein Tyrosine Kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    KRAS mutation • EGFR mutation • BRAF mutation • NRAS mutation • BRAF V600 • FGFR1 amplification • CDKN2A deletion • HRAS mutation • PTPN11 mutation • CCND1 amplification • KRAS amplification • BRAF amplification
    |
    Mekinist (trametinib) • Tafinlar (dabrafenib) • Alecensa (alectinib) • Cabometyx (cabozantinib tablet) • Stivarga (regorafenib) • Kisqali (ribociclib) • siremadlin (HDM201)
    almost2years
    Current therapeutic modalities and chemopreventive role of natural products in liver cancer: Progress and promise. (PubMed, World J Hepatol)
    Sorafenib and lenvatinib are first-line therapies, while regorafenib and ramucirumab are second-line therapy. Drug-induced toxicity is a key obstacle in the treatment of liver cancer, necessitating the development of effective and safe medications, with natural compounds such as resveratrol, curcumin, diallyl sulfide, and others emerging as promising anticancer agents. This review highlights the current status of liver cancer research, signaling pathways, therapeutic targets, current treatment strategies and the chemopreventive role of various natural products in managing liver cancer.
    Review • Journal
    |
    TGFB1 (Transforming Growth Factor Beta 1)
    |
    sorafenib • Lenvima (lenvatinib) • Stivarga (regorafenib) • Cyramza (ramucirumab)
    almost2years
    Guardant Health and AnHeart Therapeutics Announce Collaboration to Develop Guardant360 CDx and Guardant360 TissueNext as Companion Diagnostics for Taletrectinib in Advanced or Metastatic ROS1-Positive Non-Small Cell Lung Cancer (Businesswire)
    "Guardant Health Inc...announced today a strategic collaboration on the development, regulatory approval and commercialization of the Guardant360® CDx and Guardant360 TissueNext™ assays as companion diagnostics for taletrectinib in the United States and European Union....The collaboration will focus on the use of the Guardant tests for comprehensive genomic profiling to identify patients with the specific tumor mutations that are targeted by taletrectinib."
    Licensing / partnership
    |
    Guardant360® CDx • Guardant360 TissueNext™
    |
    taletrectinib (AB-106)