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QuickView for Rifapentine (compound)


PubChem
Name: rifapentine
PubChem Compound ID: 6323497
Molecular formula: C47H64N4O12
Molecular weight: 877.031 g/mol
Synonyms:
Cyclopentylrifampicin; MDL 473; KTC 1; DL-473; 3-(((4-Cyclopentyl-1-piperazinyl)imino)methyl)rifamycin; RPE; Priftin; Cyclopentyl rifampin; M000473; 3-[N-(4-Cyclopentyl-1-piperazinyl)formimidoyl]rifamycin.
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DrugBank
Identification
Name: rifapentine
Name (isomeric): DB01201
Drug Type: small molecule
Synonyms:
Cyclopentyl rifampin
Brand: Priftin
Category: Antimycobacterials, Antibiotics, Antitubercular, Leprostatic Agents
CAS number: 61379-65-5
Pharmacology
Indication: For the treatment of pulmonary tuberculosis.
Pharmacology:
Rifapentine is an antibiotic that inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme. It is bactericidal and has a very broad spectrum of activity against most gram-positive and gram-negative organisms (including Pseudomonas aerugino...
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Mechanism of Action:
Rifapentine has shown higher bacteriostatic and bactericidal activities especially against intracellular bacteria growing in human monocyte-derived macrophages. Rifapentine inhibits DNA-dependent RNA polymerase in susceptible strains of M. tuberculosis. Rifapentine acts via the inhibition of DNA-dependent RNA polymerase, leading to a suppression of...
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Absorption: Rapidly and well absorbed from the gastrointestinal tract.
Protein binding: 97.7% (bound to plasma proteins)
Biotransformation: Hepatic
Route of elimination: Following a single 600 mg oral dose of radiolabeled rifapentine to healthy volunteers (n=4), 87% of the total 14C rifapentine was recovered in the urine (17%) and feces (70%).
Clearance: Apparent Oral cl=2.51 +/- 0.14 L/h [Male tuberculosis patients who received 600 mg rifapentine in combination with isoniazid, pyrazinamide and ethambutol] Apparent Oral cl=1.69 +/- 0.41 L/h [Female tuberculosis patients who received 600 mg rifapentine in combination with isoniazid, pyrazinamide and ethambutol]
Affected organisms: Mycobacterium
Interactions
Drug interaction:
ErlotinibDecreased levels/effect of erlotinib
Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
TrazodoneThe CYP3A4 inducer, Rifapentine, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Rifapentine is initiated, discontinued or dose changed.
NorethindroneThis product may cause a slight decrease of contraceptive effect
TelithromycinRifapentine may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
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Targets


Enzymes