Drug intelligence / Profile preview

linsitinib + pemetrexed

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**OSI-906 (linsitinib) + pemetrexed** is an investigational combination therapy studied for advanced solid tumors. Linsitinib (OSI-906) is a small molecule inhibitor targeting the insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR), aiming to block signaling pathways involved in tumor cell proliferation and survival. Pemetrexed is an approved antifolate antineoplastic agent that inhibits multiple enzymes involved in folate metabolism and DNA synthesis—specifically thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT)—thereby preventing cancer cell replication. Pemetrexed is primarily indicated for non-squamous non-small cell lung cancer and malignant pleural mesothelioma[1][2][3][4][5]. The combination has been evaluated in early-phase clinical trials for advanced solid tumors but has not received regulatory approval as a combination regimen[8].

Other names
OSI-906OSI906OSI 906linsitinibpemetrexed disodium
02

Targets

DHFR (Dihydrofolate reductase)GART (GAR transformylase)IGF-1R (Insulin-like growth factor 1 receptor)INSR (Insulin receptor)TS (Thymidylate synthase)

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