Drug intelligence / Profile preview

anlotinib + pemetrexed

Development stage
Unknown
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Anlotinib + pemetrexed is a combination therapy used primarily in the treatment of non-small cell lung cancer (NSCLC), particularly in patients with advanced or metastatic disease. Anlotinib is an oral small molecule angiokinase inhibitor that targets multiple receptor tyrosine kinases involved in tumor angiogenesis and growth, including vascular endothelial growth factor receptor 1 (VEGFR1), vascular endothelial growth factor receptor 2 (VEGFR2), vascular endothelial growth factor receptor 3 (VEGFR3), platelet-derived growth factor receptor alpha (PDGFRα), platelet-derived growth factor receptor beta (PDGFRβ), fibroblast growth factor receptor 1 (FGFR1), fibroblast growth factor receptor 2 (FGFR2), fibroblast growth factor receptor 3 (FGFR3), fibroblast growth factor receptor 4 (FGFR4), as well as RET proto-oncogene, Mast/stem cell growth factor receptor Kit and Hepatocyte growth factor Receptor. Pemetrexed is a folate antimetabolite that inhibits several key folate-dependent enzymes required for DNA synthesis and cell replication—specifically thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT)[1][6]. The combination has shown efficacy as part of first-line or maintenance therapy for advanced NSCLC[3][4].

02

Targets

ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)PDGFRA (Platelet-derived growth factor receptor alpha)GART (GAR transformylase)PDGFRB (Platelet-derived growth factor receptor beta)FGFR3 (Fibroblast growth factor receptor 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)DHFR (Dihydrofolate reductase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)TS (Thymidylate synthase)

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