Drug intelligence / Profile preview

romidepsin + rifampin

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous (romidepsin), Oral (rifampin)
01

Overview

**Romidepsin + rifampin** is a combination therapy of romidepsin, a bicyclic depsipeptide histone deacetylase (HDAC) inhibitor, and rifampin, a strong CYP3A inducer and antibiotic. Romidepsin acts by inhibiting class I HDAC enzymes, leading to cell cycle arrest and apoptosis, particularly in malignant T-cells. It is approved for cutaneous T-cell lymphoma (CTCL) and peripheral T-cell lymphoma (PTCL) in patients with prior systemic therapy. Rifampin, typically used to treat tuberculosis and other bacterial infections, is a potent inducer of CYP3A4 enzymes, but in this combination, unexpectedly increases plasma exposure of romidepsin (AUC and Cmax) due to inhibition of hepatic uptake, resulting in higher risk of toxicity, especially thrombocytopenia. This combination is not approved and should generally be avoided; toxicity should be strictly monitored if used, due to the risk of enhanced romidepsin exposure[1][2][3][4].

Brand names
Istodax (romidepsin)Rifadin (rifampin)romidepsin + rifampin
Other names
romidepsin + rifampicin
02

Targets

ABCB11 (Bile salt export pump)RNAP (Bacterial dna-dependent RNA polymerase)CYP1A1 (Cytochrome P450 1A1)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)

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