Drug intelligence / Profile preview

MKC-1 + pemetrexed

Development stage
Unknown
Lead developer
CASI Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**MKC-1 + pemetrexed** is a combination therapy comprised of MKC-1, an orally available small molecule cell cycle inhibitor, and pemetrexed, a multi-targeted antifolate chemotherapeutic. MKC-1 targets microtubules, importin-β family proteins, and the AKT-mTOR pathway, disrupting mitotic spindle formation and nuclear transport, leading to cell cycle arrest and apoptosis[1][2][3]. Pemetrexed inhibits several folate-dependent enzymes involved in nucleotide synthesis, serving primarily as an antineoplastic agent[5]. The combination has been evaluated in phase 1/2 trials as a second-line therapy for advanced non-small cell lung cancer (NSCLC), showing evidence of efficacy and manageable toxicity[1][3].

Other names
MKC-1 + pemetrexed
02

Targets

GART (GAR transformylase)Kap-beta (Importin-beta family proteins)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)TUBB (Tubulin (alpha and beta subunits))

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