Drug intelligence / Profile preview

pirotinib

Development stage
Phase 2
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Pirotinib is an orally transmittable, irreversible pan-ErbB receptor tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR/HER1), HER2 (ERBB2), and HER4. It binds irreversibly to the ATP-binding sites of these receptors' intracellular segments, blocking activation of downstream signaling pathways and inhibiting tumor cell growth. Pirotinib has demonstrated antitumor activity in patients with HER2-positive advanced or metastatic breast cancer and is conditionally approved in China for use in combination with capecitabine for this indication. It has also shown efficacy in trastuzumab-resistant cases and is being investigated for other solid tumors such as non-small cell lung cancer[3][4][5][9].

Brand names
Irene
Other names
pyrotinibpyrotinib maleatepyrroltinib maleateBLTN
02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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