Last reviewed · How we verify

Capecitabine monotherapy

Zhen-Hai Lu · Phase 3 active Small molecule

Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.

Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth. Used for Metastatic colorectal cancer, Metastatic breast cancer, Gastric cancer.

At a glance

Generic nameCapecitabine monotherapy
Also known asCapecitabine
SponsorZhen-Hai Lu
Drug classFluoropyrimidine antimetabolite
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Capecitabine is an oral fluoropyrimidine carbamate that undergoes hepatic and tumor-selective conversion to 5-fluorouracil (5-FU). Once activated, 5-FU inhibits thymidylate synthase, blocking dTMP synthesis and DNA replication, while also being incorporated into RNA to disrupt protein synthesis. This dual mechanism leads to cancer cell death, particularly in rapidly dividing cells.

Approved indications

Common side effects

Key clinical trials

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape: