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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Histone deacetylase (HDAC) inhibitors
entinostat
L01XH05
Forms & Strengths
- Oral tablets: 1 mg
- Oral tablets: 5 mg
Adult Dosing
- Investigational/Off-label: 5 mg orally once weekly in combination regimens
- Clinical trials: Dosing varies based on specific oncologic protocol
Pediatric Dosing
- Safety and efficacy in pediatric patients not established
- Not recommended for use in pediatric populations outside of clinical trials
Indications
- Investigated for the treatment of advanced hormone receptor-positive breast cancer in combination with exemestane
- Investigated for various solid tumors and hematologic malignancies as a histone deacetylase (HDAC) inhibitor
Mechanism of Action
- Class I selective histone deacetylase (HDAC) inhibitor
- Inhibits HDAC isoforms 1, 2, and 3, leading to hyperacetylation of histone proteins
- Promotes chromatin remodeling, reactivation of epigenetically silenced tumor suppressor genes, and induction of apoptosis or cell cycle arrest
Contraindications
- Hypersensitivity to entinostat or any component of the formulation
- Severe hepatic impairment (depending on clinical trial protocols)
- Pregnancy and lactation due to potential teratogenicity and embryofetal toxicity
Adverse Reactions
- Fatigue
- Nausea and vomiting
- Diarrhea or constipation
- Thrombocytopenia
- Neutropenia
- Anemia
- Decreased appetite
- Elevated liver transaminases
Drug Interactions
- Co-administration with strong CYP3A4 inhibitors may alter plasma concentrations
- Co-administration with strong CYP3A4 inducers may decrease entinostat efficacy
- Potential for additive myelosuppression when combined with other cytotoxic or bone marrow-suppressive agents
Curated Content: Needs Vetting Before Put to Clinical Use