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disitamab vedotin + pyrotinib + naratinib
- Development stage
- Unknown
- Lead developer
- RemeGen
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
This is a combination therapy consisting of disitamab vedotin (an antibody-drug conjugate targeting HER2), pyrotinib (an irreversible dual pan-ErbB receptor tyrosine kinase inhibitor), and naratinib (a tyrosine kinase inhibitor). The combination is being investigated primarily for HER2-positive breast cancer with brain metastasis. Disitamab vedotin delivers the anticancer agent monomethyl auristatin E (MMAE) to HER2 receptor-expressing cells, disrupting microtubules and causing tumor destruction. Pyrotinib inhibits the autophosphorylation of HER homodimers and heterodimers, affecting the Ras/Raf/MEK/MAPK and PI3K/Akt signaling cascades. This combination approach aims to overcome resistance to prior HER2-targeted therapies.
- Brand names
- Aidixi + pyrotinib + naratinib
02
Targets
ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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