Rifapentine

Summary

Rifapentine (CHEMBL1660) is an approved small-molecule antitubercular agent (ATC J04AB05); indicated across 4 conditions including tuberculosis and pulmonary tuberculosis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J04AB05
• Indications: 4 conditions
• Clinical trials: 47
• Chemistry: 877 Da · C47H64N4O12

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1660
Name	Rifapentine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	135403821
ChEBI	CHEBI:45304
ATC	J04AB05
Molecular formula	C47H64N4O12
Molecular weight	877
InChIKey	WDZCUPBHRAEYDL-GZAUEHORSA-N

SMILES: C[C@H]1/C=C/C=C(\C(=O)NC2=C(C(=C3C(=C2O)C(=C(C4=C3C(=O)[C@](O4)(O/C=C/[C@@H]([C@H]([C@H]([C@@H]([C@@H]([C@@H]([C@H]1O)C)O)C)OC(=O)C)C)OC)C)C)O)O)/C=N/N5CCN(CC5)C6CCCC6)/C

IUPAC name: [(7S,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-26-[(E)-(4-cyclopentylpiperazin-1-yl)iminomethyl]-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.14,7.05,28]triaconta-1(29),2,4,9,19,21,25,27-octaen-13-yl] acetate

Pharmacological roles (ChEBI): antitubercular agent, leprostatic drug.

Also known as: ANTIBIOTIC DL-473IT, DL-473, KTC-1, MDL 473, MDL-473, Prifitin, Priftin, R-773, Rifapentin, Rifapentina, Rifapentine, rifapentine

Patent coverage: 3,539 distinct patent families (12,680 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 12,233 (96%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: ATP-binding cassette sub-family C member 4, Androgen receptor, Prostaglandin G/H synthase 1, Voltage-gated inwardly rectifying potassium channel KCNH2, ATP-binding cassette sub-family C member 2, ATP-binding cassette sub-family C member 3, Bile salt export pump.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KCNH2	5.92	AC50	1210	nM	CHEMBL_ACT_25117951
ABCB11	5	IC50	9910	nM	CHEMBL_ACT_18129070

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
tuberculosis	4	MONDO:0018076	MONDO:0018076
pulmonary tuberculosis	3	MONDO:0006052	EFO:1000049
HIV infectious disease	2	MONDO:0005109	EFO:0000764
osteomyelitis	0	MONDO:0005246	EFO:0003102

Clinical trials

Total trials: 47.

Phase distribution

Phase	Trials
PHASE3	14
PHASE2	9
PHASE1	9
PHASE2/PHASE3	5
PHASE1/PHASE2	4
PHASE4	3
Not specified	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06874725	PHASE4	ACTIVE_NOT_RECRUITING	Latent Tuberculosis in Type 2 Diabetes
NCT03266991	PHASE4	TERMINATED	Treatment of Latent Tuberculosis in Socially Marginalised Citizens
NCT04551573	PHASE4	WITHDRAWN	A Study of the Pharmacokinetic and Pharmacodynamic Interactions Between Bictegravir, Tenofovir Alafenamide and Rifapentine in Healthy Adult Subjects
NCT03474029	PHASE2/PHASE3	RECRUITING	Assessment of the Safety, Tolerability, and Effectiveness of Rifapentine Given Daily for LTBI
NCT03785106	PHASE3	ACTIVE_NOT_RECRUITING	Tuberculosis Preventive Therapy Among Latent Tuberculosis Infection in HIV-infected Individuals
NCT05454345	PHASE3	NOT_YET_RECRUITING	Sitafloxacin-containing Regimens for Shortening Tuberculosis Treatment
NCT06022146	PHASE3	RECRUITING	TB YOUTH - TB sYstemic Management Using One-month, Ultra-short TPT Regimen for scHool Contacts
NCT06191692	PHASE3	NOT_YET_RECRUITING	1HP Versus 3HR in the Treatment of Tuberculosis Infection in Vietnam
NCT06253715	PHASE3	RECRUITING	Shortened Regimen for Drug-susceptible TB in Children
NCT06498414	PHASE2/PHASE3	RECRUITING	Shorter and Safer Treatment Regimens for Latent TB
NCT06568484	PHASE2/PHASE3	RECRUITING	Bedaquiline Roll-out Evidence in Contacts and People Living With HIV to Prevent TB
NCT00023335	PHASE3	COMPLETED	TBTC Study 22: Efficacy of Once-Weekly Rifapentine and Isoniazid in Treatment of Tuberculosis
NCT00057122	PHASE3	COMPLETED	Tuberculosis Prevention for HIV Infected Adults
NCT01404312	PHASE3	COMPLETED	Brief Rifapentine-Isoniazid Evaluation for TB Prevention (BRIEF TB)
NCT01582711	PHASE3	COMPLETED	Study 33: Adherence to Latent Tuberculosis Infection Treatment 3HP SAT Versus 3HP DOT
NCT02208427	PHASE3	UNKNOWN	Toward a Safe and Reachable Preventive Therapy for LTBI: a Multicenter Randomized Controlled Study in Taiwan
NCT02410772	PHASE3	COMPLETED	TBTC Study 31: Rifapentine-containing Tuberculosis Treatment Shortening Regimens
NCT02563327	PHASE3	COMPLETED	Pharmacokinetic and Pharmacodynamic Study of High-Dose Rifapentine and Moxifloxacin for Treatment of Tuberculosis
NCT02735590	PHASE2/PHASE3	UNKNOWN	The Correlate of Risk Targeted Intervention Study
NCT02980016	PHASE3	COMPLETED	Evaluation of the Effect of 3HP vs Periodic 3HP vs 6H in HIV-Positive Individuals
NCT03474198	PHASE2/PHASE3	COMPLETED	Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis
NCT04094012	PHASE3	COMPLETED	Risk of SDRs Under 3HP and 1HP Regimen for LTBI
NCT05122026	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Safety and Tolerability of 1 Month Daily (1HP) and 3 Months Weekly (3HP) Isoniazid and Rifapentine With Pharmacokinetics of Dolutegravir (DTG) in Pregnant People With HIV
NCT06917495	PHASE2	NOT_YET_RECRUITING	Short-Course Anti-tuberculosis Regimens for Mild Spinal Tuberculosis
NCT07124559	PHASE1/PHASE2	NOT_YET_RECRUITING	A Study of Daily Rifapentine Combined With Isoniazid (1HP) for Tuberculosis Prevention in Children Less Than 13 Years of Age With and Without HIV
NCT07595042	PHASE2	NOT_YET_RECRUITING	A Trial of Stratified Patient-Centered Treatment Regimens for Active TB (SPECTRA-TB)
NCT00002192	PHASE2	COMPLETED	Tolerance, Safety, and Activity of Rifapentine Alone and in Combination Therapy in AIDS Patients With Mycobacterium Avium Complex Bacteremia.
NCT00023426	PHASE2	COMPLETED	TBTC Study 25: Study of the Tolerability of Higher Doses of Rifapentine in the Treatment of Tuberculosis
NCT00694629	PHASE2	COMPLETED	TBTC Study 29: Rifapentine During Intensive Phase Tuberculosis (TB) Treatment
NCT00728507	PHASE2	TERMINATED	Rifapentine Plus Moxifloxacin for Treatment of Pulmonary Tuberculosis
NCT00814671	PHASE2	COMPLETED	Study of Daily Rifapentine for Pulmonary Tuberculosis
NCT02651259	PHASE1/PHASE2	COMPLETED	Evaluating PK, Tolerability, and Safety of Rifapentine and Isoniazid in Pregnant and Postpartum Women
NCT03730181	PHASE1/PHASE2	COMPLETED	Tuberculosis Clinical Trials Consortium Study 35
NCT04272242	PHASE2	TERMINATED	Drug-Drug Interactions Between Rifapentine and Dolutegravir in HIV/LTBI Co-Infected Individuals
NCT04311502	PHASE2	TERMINATED	Clofazimine- and Rifapentine-Containing Treatment Shortening Regimens in Drug-Susceptible Tuberculosis: The CLO-FAST Study
NCT06281834	PHASE1	RECRUITING	Dolutegravir Pharmacokinetics During Weekly Rifapentine/Isoniazid for TB Prevention
NCT00460759	PHASE1	TERMINATED	Pharmacokinetic Issues of Moxifloxacin Plus Rifapentine
NCT00809718	PHASE1	COMPLETED	The Effect of Rifapentine on Raltegravir
NCT01162486	PHASE1	COMPLETED	Pharmacokinetics, Safety and Tolerability of Escalating Rifapentine Doses in Healthy Volunteers
NCT01574638	PHASE1	COMPLETED	Evaluating the Pharmacokinetics of High-Dose Rifapentine When Given as a Single Dose or in Divided Doses to Healthy Adults

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).