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disitamab vedotin + dalpiciclib + exemestane
- 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 regimen is being investigated for the treatment of HER2-low, hormone receptor-positive (HR+) metastatic breast cancer. It consists of three distinct pharmacological agents: **disitamab vedotin**, a HER2-targeted antibody-drug conjugate (ADC) that delivers a microtubule-disrupting payload (monomethyl auristatin E, MMAE) directly to cancer cells; **dalpiciclib**, a selective small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6) that halts cell cycle progression; and **exemestane**, a steroidal aromatase inhibitor that reduces estrogen production. The rationale for this triplet combination is to simultaneously inhibit HER2 signaling, the cell cycle, and the estrogen receptor pathway, potentially overcoming resistance mechanisms common in HR+/HER2-low breast cancer. The regimen is currently under evaluation in Phase 2 clinical trials sponsored by The First Affiliated Hospital of Wenzhou Medical University.
- Brand names
- AiditaiAi Rui Yi
- Other names
- RC48-ADCRC-48-ADCRC 48-ADCSHR-6390SHR6390SHR 6390
02
Targets
CYP19A1 (Aromatase)CDK6 (Cyclin-dependent kinase 6)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK4 (Cyclin-dependent kinase 4)TUBB (Tubulin (alpha and beta subunits))
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