Drug intelligence / Profile preview

BLU-451 + carboplatin + pemetrexed

Development stage
Unknown
Lead developer
Blueprint Medicines
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**BLU-451 + carboplatin + pemetrexed** is an investigational three-drug combination studied primarily in the context of **non-small cell lung cancer (NSCLC)**, particularly cases driven by atypical or Exon 20 insertion mutations of the **Epidermal Growth Factor Receptor (EGFR)** gene. - **BLU-451** is a covalent, CNS-penetrant, oral small molecule inhibitor designed to selectively target EGFR Exon 20 insertion mutations while sparing wild-type EGFR, thereby aiming to minimize toxicity and maximize efficacy in relevant cancer subtypes[1][3][5]. - **Carboplatin** is a platinum-based chemotherapeutic agent that promotes DNA crosslinking and induces apoptosis in rapidly dividing cells[2][4][6][8]. - **Pemetrexed** is an antifolate antineoplastic that disrupts folate-dependent metabolic processes critical for cell replication, leading to inhibition of DNA and RNA synthesis[2][4][6][8]. The combination regimen is under investigation for the treatment of advanced, EGFR-mutant NSCLC, including in patient populations with brain metastases, based on the CNS penetration of BLU-451 and the well-established efficacy of pemetrexed and carboplatin in NSCLC[3][5][6]. BLU-451 has been developed by Blueprint Medicines.

Other names
pemetrexed and carboplatin
02

Targets

EGFR ex20ins (Epidermal growth factor receptor exon 20 mutant)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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