repotrectinib

ROS1-TRK-ALK inhibitor

Also Known As:

(1Z)-6-Fluoro-3,11-dimethyl-10-oxa-2,13,17,18,21-pentaazatetracyclo(13.5.2.04,9.018,22)docosa-1,4,6,8,15,19,21-heptaen-14-one; 1,15-Etheno-1H-pyrazolo(4,3-f)(1,4,8,10)benzoxatriazacyclotridecin-4(5H)-one, 11-fluoro-2,6,7,13-tetrahydro-7,13-dimethyl-, (14Z)-

Networked: 10 relevant articles (1 outcomes, 4 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Drilon, Alexander: 3 articles (12/2021 - 10/2018)
2.	Deng, Wei: 2 articles (12/2021 - 10/2018)
3.	Rogers, Evan: 2 articles (12/2021 - 10/2018)
4.	Stopatschinskaja, Shanna: 2 articles (12/2021 - 10/2018)
5.	Zhai, Dayong: 2 articles (12/2021 - 10/2018)
6.	Cho, Byoung Chul: 2 articles (01/2020 - 10/2018)
7.	Cui, J Jean: 2 articles (01/2020 - 10/2018)
8.	Arai, Sachiko: 1 article (07/2022)
9.	Fukuda, Koji: 1 article (07/2022)
10.	Kotani, Hiroshi: 1 article (07/2022)

Related Diseases

1.	Neuroblastoma 12/18/2019 - "In the present study we investigated the effects of repotrectinib in a neuroblastoma setting in vitro and in vivo. " 11/01/2021 - "Repotrectinib (TPX-0005) is a multikinase inhibitor that targets ALK, TRK, JAK2/STAT, and Src/FAK, which have all been implicated in the pathogenesis of neuroblastoma. " 11/01/2021 - "Translational Strategies for Repotrectinib in Neuroblastoma." 12/18/2019 - "Our results show that repotrectinib is capable of inhibiting signaling activity of a range of ALK mutant variants found in neuroblastoma patients and importantly it exhibits strong antitumor effects in a xenograft model of neuroblastoma." 12/18/2019 - "The in vivo effect of repotrectinib was also analyzed in a neuroblastoma xenograft model. "
2.	Neoplasms (Cancer) 10/21/2021 - "Repotrectinib shows high activity against ROS1/TRK/ALK fusion-positive cancers in preclinical studies. " 12/01/2021 - "Durable responses were observed in TKI-naïve and -pretreated patients with NTRK + cancers treated with repotrectinib (NCT03093116). " 12/01/2021 - "Repotrectinib caused tumor regression in LMNA-NTRK1 xenograft models harboring GKM, SFM, xDFG, and GKM + SFM compound mutations. " 10/01/2018 - "Importantly, repotrectinib exhibits activity against a variety of solvent-front substitutions in vitro and in vivo As clinical proof of concept, in an ongoing first-in-human phase I/II trial, repotrectinib achieved confirmed responses in patients with ROS1 or NTRK3 fusion-positive cancers who had relapsed on earlier-generation TKIs due to ROS1 or TRKC solvent-front substitution-mediated resistance.Significance" 11/01/2023 - "We report Bemcentinib and Repotrectinib, formerly prescribed for cancer, as potential inhibitors of the CK1 δ. "
3.	Neoplasm Metastasis (Metastasis) 01/01/2020 - "Intracranial antitumor activity of repotrectinib was evaluated in a brain-metastasis mouse model. " 07/01/2022 - "We further demonstrate that the triplet combination of repotrectinib, EGFR inhibitor, and MEK inhibitor could sensitize M3B cells in vitro as well as in a brain metastasis model. " 07/01/2022 - "In the present study, we established entrectinib-resistant tumor cells (M3B) in a brain metastasis model inoculated with NTRK1-rearranged KM12SM cells and examined the sensitivity of M3B cells to repotrectinib. "
4.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 11/16/2023 - "Repotrectinib's Clinical Benefit and Its Brain Penetration in a Patient with Meningeal Carcinomatosis from G2032R-Mutated ROS-1 Positive Non-Small Cell Lung Cancer." 01/01/2020 - "Repotrectinib Exhibits Potent Antitumor Activity in Treatment-Naïve and Solvent-Front-Mutant ROS1-Rearranged Non-Small Cell Lung Cancer." 11/16/2023 - "In this work, we report on a clinically significant response of meningeal carcinomatosis to repotrectinib in a woman with a heavily pretreated ROS1-rearranged non-small cell lung cancer (NSCLC) that harbored the concomitant solvent front G2032R mutation. "
5.	Meningeal Carcinomatosis 11/16/2023 - "Meningeal carcinomatosis has a higher incidence in oncogene addicted NSCLC due to increased life expectancy, yet no report has ever documented the activity of repotrectinib in this context. " 11/16/2023 - "Repotrectinib's Clinical Benefit and Its Brain Penetration in a Patient with Meningeal Carcinomatosis from G2032R-Mutated ROS-1 Positive Non-Small Cell Lung Cancer." 11/16/2023 - "In this work, we report on a clinically significant response of meningeal carcinomatosis to repotrectinib in a woman with a heavily pretreated ROS1-rearranged non-small cell lung cancer (NSCLC) that harbored the concomitant solvent front G2032R mutation. "

Related Drugs and Biologics

1.	Solvents
2.	entrectinib
3.	selitrectinib
4.	Mitogen-Activated Protein Kinase Kinases (MEKs)
5.	Crizotinib
6.	ceritinib
7.	bemcentinib
8.	ensartinib
9.	larotrectinib
10.	lorlatinib

Related Therapies and Procedures

1.	Drug Therapy (Chemotherapy)