Kesaila Trilaciclib Hydrochloride for Injection

1. Indications and Usage
Extensive-Stage Small Cell Lung Cancer (ES-SCLC):
To reduce the incidence of myelosuppression in adult patients with ES-SCLC receiving an etoposide injection and a platinum agent (cisplatin or carboplatin)-based chemotherapy regimen.
Metastatic Triple-Negative Breast Cancer (mTNBC):
To reduce the incidence of myelosuppression in adult patients with mTNBC receiving a gemcitabine injection and carboplatin-based chemotherapy regimen.
Advanced Colorectal Cancer (aCRC):
To reduce the incidence of myelosuppression in adult patients with aCRC receiving a FOLFOX-based chemotherapy regimen.
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Timing of Administration:
Must be administered within 4 hours prior to each dose of chemotherapy.
Recommended Dosage:
Standard Dose: 240 mg/m².
Infusion Duration: Administer as an IV infusion over 30 minutes.
Critical Administration Instructions:
No Premedication Required: Prophylactic corticosteroids or antihistamines are not required prior to administration.
Preparation: Reconstitute and dilute in 0.9% Sodium Chloride Injection, USP.
3. Mechanism of Action
CDK4/6 Inhibition:
Trilaciclib is a potent, selective, and reversible CDK4/6 inhibitor.
G1 Phase Cell Cycle Arrest:
It transiently arrests hematopoietic stem and progenitor cells (HSPCs) in the G1 phase of the cell cycle.
Therapeutic Result: By putting healthy bone marrow cells into a temporary “hibernation” (G1 phase), they become less susceptible to chemotherapy drugs that target rapidly dividing (S/G2 phase) cells. This protects the bone marrow from chemotherapy-induced damage without inhibiting the antitumor efficacy of the chemotherapy.
4. Safety and Warnings
Infusion-Related Reactions:
Infusion-related reactions may occur. Monitor patients during infusion.
Hyperglycemia:
Transient hyperglycemia has been observed. Monitor blood glucose levels.
Contraindications:
There are no contraindications listed in the label for general use, but caution is advised in patients with uncontrolled diabetes or active infections.
5.Adverse Reactions
Most Common:
Fatigue, constipation, nausea, increased transaminases, increased creatinine, headache, and neutropenia (though it reduces incidence compared to chemotherapy alone, it is still a monitored parameter).
6.Drug Interactions
Transporter Substrates:
Trilaciclib is a substrate and inhibitor of OATP1B1, OATP1B3, OCT1, and OCT2.
Action: Use caution when co-administered with drugs like Metformin (may increase metformin exposure) or chemotherapies that are substrates of these transporters (e.g., Cisplatin).
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Trilaciclib Hydrochloride.
Appearance: Lyophilized cake or powder, white to off-white.
Packaging: Single-dose vial (300 mg).
Storage: Store in a refrigerator at 2°C to 8°C (36°F to 46°F).