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disitamab vedotin + pyrotinib
- 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 combination therapy consists of disitamab vedotin (RC48) and pyrotinib. Disitamab vedotin is an antibody-drug conjugate (ADC) developed by RemeGen, featuring a humanized anti-HER2 monoclonal antibody (hertuzumab) conjugated to the microtubule-disrupting agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline linker. Pyrotinib, developed by Hengrui Medicine, is an orally available, irreversible pan-ErbB receptor tyrosine kinase inhibitor (TKI) that targets HER1 (EGFR), HER2, and HER4. The combination is currently being evaluated in Phase II clinical trials, such as those led by The First Affiliated Hospital with Nanjing Medical University, as a neoadjuvant treatment for patients with previously untreated HER2-positive early breast cancer. Preclinical evidence suggests that pyrotinib may enhance the efficacy of disitamab vedotin by upregulating HER2 expression on the tumor cell surface, thereby facilitating increased ADC binding and internalization.
- Brand names
- AidixiIrely
- Other names
- RC48-ADCRC-48-ADCRC 48-ADChertuzumab vedotindisitamb vedotin + pyrotinib
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))
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