Drug intelligence / Profile preview

taletrectinib + carboplatin + pemetrexed

Development stage
Unknown
Lead developer
Nuvation Bio
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination therapy comprising **taletrectinib**, **carboplatin**, and **pemetrexed**. - **Taletrectinib** is a small molecule inhibitor of the tyrosine kinase domain of ROS1 and NTRK, being developed primarily for the treatment of ROS1-positive non-small cell lung cancer (NSCLC). Its mechanism involves selective inhibition of oncogenic ROS1 and NTRK kinases, blocking downstream signaling associated with tumor growth and survival. - **Carboplatin** is a platinum-based chemotherapeutic agent that causes DNA crosslinking and strand breaks, leading to apoptosis in rapidly dividing tumor cells[3]. - **Pemetrexed** is an antifolate antineoplastic agent that inhibits several enzymes involved in folate metabolism and DNA synthesis, disrupting nucleotide synthesis and cell division[3]. This triple combination is under investigation for advanced or metastatic NSCLC with relevant oncogenic drivers.

02

Targets

NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)NTRK1 (Tropomyosin-related receptor kinase A)TS (Thymidylate synthase)GART (GAR transformylase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DHFR (Dihydrofolate reductase)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)DNA

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