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pyrotinib plus capecitabine

Henan Cancer Hospital · Phase 3 active Small molecule

Pyrotinib is a tyrosine kinase inhibitor that targets the HER2/neu receptor, while capecitabine is a prodrug of fluorouracil, an antimetabolite that interferes with DNA synthesis.

Pyrotinib is a tyrosine kinase inhibitor that targets the HER2/neu receptor, while capecitabine is a prodrug of fluorouracil, an antimetabolite that interferes with DNA synthesis. Used for Advanced or metastatic breast cancer with HER2 overexpression, Metastatic colorectal cancer.

At a glance

Generic namepyrotinib plus capecitabine
Also known asSHR1258, Irene
SponsorHenan Cancer Hospital
Drug classTyrosine kinase inhibitor, Antimetabolite
TargetHER2/neu, Thymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Pyrotinib works by binding to the HER2/neu receptor, preventing its activation and subsequent signaling pathways that promote cell growth and survival. Capecitabine, on the other hand, is converted into fluorouracil, which is then phosphorylated into fluorodeoxyuridine monophosphate (FdUMP) and fluorodeoxyuridine triphosphate (FdUTP). These metabolites inhibit thymidylate synthase, leading to the depletion of thymidine and ultimately, cell death.

Approved indications

Common side effects

Key clinical trials

Primary sources

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

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