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imetelstat

L01XX80

Forms & Strengths

Imetelstat is available as a sterile solution for intravenous injection
Supplied in single-dose vials containing 8.5 mg or 42.5 mg of imetelstat

Adult Dosing

The recommended dose is 9.4 mg/kg administered intravenously over 2 hours
Dose is administered on days 1, 8, and 15 of a 28-day cycle, for a maximum of 2 cycles

Pediatric Dosing

Safety and efficacy have not been established in pediatric patients
Use in pediatric patients is not recommended due to potential toxicity

Indications

Treatment of adult patients with intermediate-2 or high-risk myelofibrosis who have not responded to or are not eligible for other therapies
Treatment of adult patients with essential thrombocythemia who have not responded to or are not eligible for other therapies

Mechanism of Action

Imetelstat is a potent inhibitor of telomerase, an enzyme necessary for cancer cell proliferation
Inhibition of telomerase leads to telomere shortening, causing cell death in cancer cells

Contraindications

Hypersensitivity to imetelstat or any component of the formulation
Severe neutropenia or thrombocytopenia

Adverse Reactions

Neutropenia, thrombocytopenia, anemia, and lymphopenia
Fatigue, gastrointestinal symptoms, and infusion-related reactions

Drug Interactions

CYP3A4 inhibitors may increase imetelstat exposure
Imetelstat may increase the exposure of CYP3A4 substrates

Curated Content: Needs Vetting Before Put to Clinical Use