Drug intelligence / Profile preview

afatinib + cisplatin + paclitaxel

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

Overview

This is a **combination chemotherapy regimen** consisting of three agents: **afatinib**, an oral irreversible ErbB family blocker; **cisplatin**, a platinum-based DNA cross-linking agent; and **paclitaxel**, a microtubule-stabilizing taxane. Afatinib inhibits epidermal growth factor receptor (EGFR) family tyrosine kinases, blocking downstream signaling and resulting in reduced cell proliferation and increased apoptosis. Cisplatin forms DNA adducts leading to apoptosis in rapidly dividing cells. Paclitaxel stabilizes microtubules and prevents mitosis. This combination has been investigated in solid tumors—including advanced head and neck cancers and other advanced solid tumors—with the maximum tolerated dose of afatinib established as 20 mg in combination with cisplatin (50 or 75 mg/m²) and paclitaxel (175 mg/m²). Preemptive management of side effects (mainly diarrhea and nausea) is important for maintaining safety and tolerability. The regimen has shown antitumor activity with disease control in several tumor types[1].

02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)TUBB (Tubulin (alpha and beta subunits))DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR (Epidermal growth factor receptor)

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