Drug intelligence / Profile preview

ABT-751 + capecitabine + irinotecan

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

Overview

ABT-751 + capecitabine + irinotecan is an investigational combination therapy composed of three agents, each with distinct mechanisms of action, primarily studied for the treatment of advanced or refractory cancers such as colorectal cancer. - **ABT-751** is an orally bioavailable small molecule sulfonamide that binds to the colchicine-binding site on beta-tubulin, inhibiting microtubule polymerization and disrupting cell division. It also exhibits antivascular properties by affecting tumor vasculature and perfusion[4][6][7]. - **Capecitabine** is an oral prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in vivo; it acts as a pyrimidine antimetabolite inhibiting thymidylate synthase, thereby interfering with DNA synthesis. - **Irinotecan** is a topoisomerase I inhibitor that prevents DNA unwinding and replication by stabilizing the cleavable complex between topoisomerase I and DNA. This combination leverages complementary cytotoxic mechanisms—microtubule disruption (ABT-751), inhibition of DNA synthesis (capecitabine/5-FU), and interference with DNA repair/replication (irinotecan)—to enhance antitumor efficacy. The regimen has been evaluated in clinical trials for solid tumors including colorectal cancer[1].

02

Targets

TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)TUBB (Tubulin (alpha and beta subunits))

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