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trilaciclib + topoisomerase I inhibitor type ADC drugs
- Development stage
- Unknown
- Lead developer
- G1 Therapeutics
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Trilaciclib is a first-in-class, highly potent, and reversible small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). It is administered intravenously prior to chemotherapy to induce transient G1 cell cycle arrest in hematopoietic stem and progenitor cells (HSPCs), thereby protecting them from chemotherapy-induced myelosuppression (myeloprotection). This specific combination regimen involves the use of trilaciclib in conjunction with antibody-drug conjugates (ADCs) that utilize topoisomerase I inhibitors as their cytotoxic payload (such as deruxtecan or govitecan). The combination is currently being investigated in Phase II clinical trials, notably by Tianjin Medical University Cancer Institute and Hospital, to evaluate its efficacy in reducing bone marrow toxicity in cancer patients treated with these potent ADC therapies.
- Brand names
- Cosela
- Other names
- Trilaciclib and Topoisomerase I inhibitor type ADC drugs
02
Targets
SLC47A1 (Multidrug and toxin extrusion transporter 1)TOP1 (DNA Topoisomerase I)MAGEA8 (Melanoma-associated antigen 8)CDK6 (Cyclin-dependent kinase 6)CDK7OCT2 (Organic cation transporter 2)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)MATE2-K (Multidrug and toxin extrusion protein 2)CDK9 (Cyclin-dependent kinase 9)CDK5 (Cyclin-dependent kinase 5)
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