e-Drug3D

1652

M RIFAPENTINE

INN
RIFAPENTINE

(is an active metabolite)

cas 79039-56-8

CLASS

ANTIINFECTIVES
TUBERCULOSTATIC
ANTIBIOTIC
RIFAMYCIN ANTIMYCOBACTERIALS
INHIBITS DNA-DEPENDENT RNA POLYMERASE

ROUTE (list)

ATC code

J04AB05

PK parameters

Tmax 11.2 HOUR
Cmax 7.5 MICROMOLAR
PPB 93.2 PERCENT
t1/2 13 HOUR

Target

TARGET DNA-DIRECTED RNA POLYMERASE

DrugCentral

Bacterial DNA-directed RNA polymerase UNIPROT P0A7Z4 rpoA

Download SDF file

Rifamycin, 3-[[(4-cyclopentyl-1-piperazinyl)imino]methyl]-25-O-deacetyl-

Formula:
C45H62N4O11

Calculated chemical properties:

MW 834.99
NB_atoms 60
XLogP 5.08
PSA 192.136
NB_HD 7
NB_HA 15
fsp3 0.58
Lipinski(0=no;1=yes) 0

FDA
-

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

841

RIFAPENTINE

INN
RIFAPENTINE

(has an active metabolite)

cas 61379-65-5

CLASS

ANTIINFECTIVES
TUBERCULOSTATIC
ANTIBIOTIC
RIFAMYCIN ANTIMYCOBACTERIALS
INHIBITS DNA-DEPENDENT RNA POLYMERASE

ROUTE (list)

ORAL

ATC code

J04AB05

PK parameters

F 70 PERCENT
Tmax 5.5 HOUR
Cmax 17.1 MICROMOLAR
VD 70 LITER
Cl 2.03 LITER / HOUR
PPB 97.7 PERCENT
t1/2 13 HOUR

Target

TARGET DNA-DIRECTED RNA POLYMERASE

PDB
2A69 (CRYSTAL STRUCTURE OF THE T. THERMOPHILUS RNA POLYMERASE HOLOENZYME IN COMPLEX WITH ANTIBIOTIC RIFAPENTIN)

Ligand code = RPT (link to the list of PDB complexes)

Download experimental 3D coordinates of RPT with added hydrogens

DrugCentral

Bacterial DNA-directed RNA polymerase UNIPROT P0A7Z4 rpoA

Download SDF file

Rifamycin, 3-[[(4-cyclopentyl-1-piperazinyl)imino]methyl]-

Formula:
C47H64N4O12

Calculated chemical properties:

MW 877.02
NB_atoms 63
XLogP 5.65
PSA 197.062
NB_HD 6
NB_HA 16
fsp3 0.57
Lipinski(0=no;1=yes) 0

FDA
NDA 021024 (label) INN (RIFAPENTINE) PRIFTIN (SANOFI AVENTIS US) APPROVAL= AP YEAR= 1998
NDA 217042 (pdf not found) INN (RIFAPENTINE) RIFAPENTINE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2026