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Trilaciclib

Brand: Cosela

CDK4/6 Inhibitor, Myeloprotectant

Chemotherapy AdjunctCytoprotectant

ApprovedPrescription Only

Overview

Trilaciclib is a first-in-class, short-acting, reversible cyclin-dependent kinase 4/6 (CDK4/6) inhibitor administered intravenously prior to chemotherapy to protect bone marrow cells from damage. It is used to reduce the incidence of chemotherapy-induced myelosuppression in adult patients receiving certain chemotherapy regimens for extensive-stage small-cell lung cancer (ES-SCLC). Trilaciclib temporarily stops cell cycle progression in the hematopoietic stem and progenitor cell compartment during chemotherapy administration, thus reducing their susceptibility to damage.

Primary Use

Trilaciclib is used to decrease the frequency of chemotherapy-induced myelosuppression in patients receiving specific chemotherapy regimens for extensive-stage small-cell lung cancer.

Pharmacokinetics

Within 1 hour

Onset

3-5 hours

Half-Life

240 mg

Max Dose

Liver (CYP3A4)

Metabolism

Clinical Applications

Approved Indications

Reduction of the incidence of chemotherapy-induced myelosuppression in adult patients when administered prior to a platinum/etoposide-containing regimen or topotecan-containing regimen for extensive-stage small cell lung cancer (ES-SCLC)

Reduction in the incidence of chemotherapy-induced myelosuppression in adult patients receiving certain chemotherapy regimens for early-stage breast cancer administered prior to docetaxel, doxorubicin, and cyclophosphamide (TAC) chemotherapy

Off-Label Uses

Myelosuppression prevention in patients receiving other myelotoxic chemotherapy regimens (e.g., for ovarian cancer, bladder cancer)

Mitigation of myelosuppression in patients undergoing hematopoietic stem cell transplantation

Side Effects

Neutropenia

Anemia

Leukopenia

Thrombocytopenia

Lymphopenia

Drug Interactions

Strong CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole)

High

Outcome:

Increased trilaciclib exposure

Mechanism:

Inhibition of CYP3A4-mediated metabolism

Moderate CYP3A4 Inhibitors (e.g., erythromycin)

Moderate

Outcome:

Increased trilaciclib exposure

Mechanism:

Partial inhibition of CYP3A4-mediated metabolism

Antacids

Low

Outcome:

Potentially decreased trilaciclib absorption

Mechanism:

Changes in gastric pH

AI Predictions & Insights

Innovation Forecast

Most likely new formulation: Oral formulation (2026, 60% confidence)

Regulatory Outlook

Based on current usage and clinical trial data, there is a 70% likelihood of expanded indications for trilaciclib in other chemotherapy regimens within the next 5 years.

Classification & Chemical Information

Primary Classification

CDK4/6 Inhibitor, Myeloprotectant

Chemical Class

Pyrido[2,3-d]pyrimidin-7-one

Trilaciclib (Cosela): Uses, Interactions, and Mechanism of Action