Drug intelligence / Profile preview

t900607-sodium

Development stage
Phase 2
Lead developer
Amgen
Modality
Small Molecules
Administration
Intravenous
01

Overview

T900607-sodium is a pentafluorophenylsulfonamide derivative with potential antineoplastic activity. It functions as a tubulin inhibitor that disrupts microtubule polymerization by binding irreversibly to colchicine binding sites on β-tubulin. Specifically, it causes a covalent modification of β1, β2, and β4 isotypes of β-tubulin. Unlike some other tubulin inhibitors, T900607 is not a substrate for p-glycoprotein drug pump and has shown activity in multidrug resistant (MDR) models in preclinical studies. In human tumor xenograft studies, it demonstrated activity against various cancer types including mammary (MX-1, MCF-7, MCF-7/ADR), ovarian (C13), colon (HT 29), renal carcinoma (Caki-1), and lymphoblastic leukemia, with efficacy comparable or superior to vinblastine, doxorubicin and paclitaxel. However, in clinical trials, T900607-sodium showed significant toxicity, including thrombocytopenia, nausea/vomiting, fatigue, and cardiac toxicity.

Other names
T-900607T900607T 900607T 607T607T-607
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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