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carboplatin + paclitaxel + varlitinib
- Development stage
- Unknown
- Lead developer
- ASLAN Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination regimen consisting of three drugs: - **Carboplatin**: A platinum-based chemotherapy agent that causes DNA crosslinking and apoptosis in rapidly dividing cells. - **Paclitaxel**: A microtubule-stabilizing agent that inhibits cell division by preventing microtubule depolymerization. - **Varlitinib**: An oral, highly potent small-molecule pan-HER inhibitor targeting HER1 (EGFR), HER2, and HER4. Varlitinib blocks the kinase activity of these receptors, inhibiting downstream signaling pathways involved in tumor growth and survival. The triplet combination has been investigated in phase Ib studies for advanced or metastatic solid tumors, including HER2-positive breast cancer. However, the full triplet was found to be intolerable due to dose-limiting toxicities such as neutropenia and electrolyte disturbances; development focused instead on varlitinib plus paclitaxel[1][2]. The regimen was explored primarily as a potential neoadjuvant therapy for HER2+ breast cancer.
- Other names
- paclitaxel + carboplatin + ASLAN001
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))ERBB4 (Erb-b2 receptor tyrosine kinase 4)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)
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