Varlitinib is an oral, selective, reversible, small molecule tyrosine kinase inhibitor of both ErbB-2 (Her-2/neu) and EGFR. Over-expression of ErbB-2 and EGFR receptors in tumors is predictive of poor prognosis... Varlitinib has shown significant anti-tumor activity in preclinical models of human breast, lung, and epidermal carcinoma tumors.
- Mechanism
- Curator reviewed
Varlitinib is an orally active, reversible, enzymatic and cellular inhibitor, with nanomolar potency, of the key growth factor receptor tyrosine kinases ErbB-2 and EGFR. The compound possesses improved physiochemical properties relative to compounds directed at these targets currently in clinical development, and provides superior exposure and equivalent or greater efficacy in animal models of human cancer. Currently, there is no single drug on the market that selectively inhibits both ErbB-2 and EGFR. Varlitinib, which concurrently inhibits the molecular targets of the drugs Herceptin(R) (ErbB-2) and Erbitux(R) (EGFR), may provide enhanced efficacy in the treatment of cancer patients.
- Primary indication
- Investigated for use/treatment in cancer/tumors (unspecified).Curator reviewed
- Formula / weight
- C22H19ClN6O2S · 466.94 g/mol (avg)
- Code names
- AR-00334543 · ARRY-334543 · ARRY-543 · ASLAN-001
Resolves to
UWXSAYUXVSFDBQ-CYBMUJFWSA-NSMILESC[C@@H]1COC(NC2=CC=C3N=CN=C(NC4=CC=C(OCC5=NC=CS5)C(Cl)=C4)C3=C2)=N1What you can answer from here — as of September 13, 2026
Which drugs share a target with Varlitinib, and which of those have an active Phase 3 trial?
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