Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C37H47NO12 |
Molecular Weight | 697.77 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@]1([H])/C(/[H])=C(\[H])/C(/[H])=C(/C)\C(=Nc2cc(c3c(c(c(C)c4c3C(=O)[C@@](C)(O/C(/[H])=C(\[H])/[C@@]([H])([C@@]([H])(C)[C@]([H])([C@]([H])(C)[C@@]([H])([C@]([H])(C)[C@@]1([H])O)O)OC(=O)C)OC)O4)O)c2O)O)O
InChI
InChIKey=HJYYPODYNSCCOU-ODRIEIDWSA-N
InChI=1S/C37H47NO12/c1-16-11-10-12-17(2)36(46)38-23-15-24(40)26-27(32(23)44)31(43)21(6)34-28(26)35(45)37(8,50-34)48-14-13-25(47-9)18(3)33(49-22(7)39)20(5)30(42)19(4)29(16)41/h10-16,18-20,25,29-30,33,40-44H,1-9H3,(H,38,46)/b11-10+,14-13+,17-12-/t16-,18+,19+,20+,25-,29-,30+,33+,37-/m0/s1
Molecular Formula | C37H47NO12 |
Molecular Weight | 697.77 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Rifamycin SV is a derivative of antibiotic rifamycin B (the natural fermentation product of S. mediterranei broths). The primary target of rifampicin on whole bacteria is the synthesis of RNA. Rifamycin belongs to the ansamycin class of antibacterial drugs and acts by inhibiting the beta subunit of the bacterial DNA-dependent RNA polymerase, blocking one of the steps in DNA transcription. This results in inhibition of bacterial synthesis and consequently growth of bacteria. Rifampicin exhibits bactericidal activity on Gram-positive and Gram-negative bacteria and on mycobacteria. Rifamycin SV MMX® (AEMCOLO), a non-absorbable rifamycin antibiotic formulated using the multi-matrix system, was designed to exhibit its pharmacological action on the distal small intestine and colon. AEMCOLO is indicated for the treatment of travelers’ diarrhea (TD) caused by non-invasive strains of Escherichia coli in adults.
Originator
Sources: Sensi P., Margalith P., Timbal M.T. Farmaco (Ed. Sci.) 1959;14:146 |
Sensi P., Greco, A.M., Ballotta, R. Antimicrob. Ag. Chemother. 1959;60:262-70
Curator's Comment:: Rifamycin family of antibiotics originally isolated from the fermentation broths of S. mediterranei.
https://www.ncbi.nlm.nih.gov/pubmed/4562808
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | AEMCOLO Approved UseAEMCOLO is a rifamycin antibacterial indicated for the treatment of travelers’ diarrhea caused by noninvasive strains of Escherichia coli in adults Launch Date1.54223994E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
36025 ng/mL |
250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIFAMYCIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
8.72 ng/mL |
388 mg 2 times / day multiple, oral dose: 388 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RIFAMYCIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11865.21 ng × h/mL |
250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIFAMYCIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.04 h |
250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
RIFAMYCIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20% |
388 mg 2 times / day multiple, oral dose: 388 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RIFAMYCIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 199 Sources: |
Other AEs: Constipation... Other AEs: Constipation (3.5%) Sources: |
388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 420 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 420 Sources: |
Other AEs: Headache, Dyspepsia... Other AEs: Headache (3.3%) Sources: Dyspepsia (<2%) |
388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 619 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 619 Sources: |
Disc. AE: Abdominal pain, Pyrexia... AEs leading to discontinuation/dose reduction: Abdominal pain (0.5%) Sources: Pyrexia (0.3%) |
400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Other AEs: Abdominal distension, Arthralgia... Other AEs: Abdominal distension (0.5%) Sources: Arthralgia (0.5%) Muscle spasms (1%) Fatigue (1%) Bronchitis (1%) Nasopharyngitis (0.5%) Parasitic gastroenteritis (1%) Pharyngitis (0.5%) Urinary tract infection (1%) Dysmenorrhea (1.5%) Dysuria (1%) Dizziness (0.5%) Conjunctivitis (1%) |
400 mg 2 times / day multiple, oral Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (1%) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Constipation | 3.5% | 388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 199 Sources: |
Headache | 3.3% | 388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 420 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 420 Sources: |
Dyspepsia | <2% | 388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 420 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 420 Sources: |
Pyrexia | 0.3% Disc. AE |
388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 619 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 619 Sources: |
Abdominal pain | 0.5% Disc. AE |
388 mg 2 times / day multiple, oral Recommended Dose: 388 mg, 2 times / day Route: oral Route: multiple Dose: 388 mg, 2 times / day Sources: |
unhealthy, 36.2 years (range: 18 - 87 years) n = 619 Health Status: unhealthy Condition: travelers’ diarrhea Age Group: 36.2 years (range: 18 - 87 years) Sex: M+F Population Size: 619 Sources: |
Abdominal distension | 0.5% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Arthralgia | 0.5% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Dizziness | 0.5% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Nasopharyngitis | 0.5% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Pharyngitis | 0.5% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Bronchitis | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Conjunctivitis | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Dysuria | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Fatigue | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Muscle spasms | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Parasitic gastroenteritis | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Urinary tract infection | 1% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Dysmenorrhea | 1.5% | 400 mg 2 times / day multiple, oral Recommended Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy n = 199 Health Status: unhealthy Condition: travelers’ diarrhea Sex: M+F Population Size: 199 Sources: |
Diarrhea | 1% Disc. AE |
400 mg 2 times / day multiple, oral Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210910Orig1s000MultidisciplineR.pdf#page=184 Page: 184.0 |
yes [EC50 11.1 uM] | |||
yes [IC50 34.4 uM] | ||||
yes [IC50 6.5 uM] | ||||
yes [Ki 2 uM] | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | unlikely Comment: Co-administration of rifamycin SV MMX with P-gp inhibitors is not expected to result in a clinically relevant increase in the systemic exposure of rifamycin SV based on the following: i) poor drug solubility; ii) wide safety margin in relation to systemic exposures observed with i.v. rifamycin SV, iii) limited 3-day treatment duration; and iv) colonic release (P-gp levels lower in colon and distal to site of most oral drugs’ absorption (i.e., duodenum and jejunum). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210910Orig1s000MultidisciplineR.pdf#page=192 Page: 192.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Inhibition of sandfly fever Sicilian virus (Phlebovirus) replication in vitro by antiviral compounds. | 1997 Sep-Oct |
|
Characterization of the mouse bile salt export pump overexpressed in the baculovirus system. | 2001 May |
|
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. | 2002 Jul |
Sample Use Guides
The recommended dosage of AEMCOLO (rifamycin) delayed-release tablets is 388 mg (two tablets) orally twice daily for three days
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21149623
Rifamycin SV demonstrated similar antimicrobial activity levels against the Enterobacteriaceae, with MIC₅₀ values ranging from 32 to 128 μg/ml for all but one strain (an enterotoxigenic Escherichia coli at >512 μg/ml). For non-Enterobacteriaceae strains, MIC₅₀ values ranged from 2 to 8 μg/ml, with the exception of Campylobacter spp., for which all strains had MIC values of >512 μg/ml. Rifamycin SV also demonstrated excellent activity (MIC₅₀ of ≤ 0.03 μg/ml) against most C. difficile strains (including one hypervirulent NAP1 strain), and this activity was even superior to the potency observed for vancomycin, metronidazole, and rifaximin.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 11:54:49 UTC 2021
by
admin
on
Sat Jun 26 11:54:49 UTC 2021
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Record UNII |
DU69T8ZZPA
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Record Status |
Validated (UNII)
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Record Version |
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WHO-VATC |
QJ04AB03
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WHO-ATC |
S01AA16
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WHO-VATC |
QJ54AB03
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WHO-ATC |
J04AB03
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NCI_THESAURUS |
C280
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WHO-ATC |
S02AA12
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WHO-VATC |
QS01AA16
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WHO-VATC |
QS02AA12
Created by
admin on Sat Jun 26 11:54:50 UTC 2021 , Edited by admin on Sat Jun 26 11:54:50 UTC 2021
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Code System | Code | Type | Description | ||
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SUB10310MIG
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Rifamycin
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C29406
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4817
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DB11753
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C023808
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230-273-3
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6998-60-3
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35616
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M9613
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PRIMARY | Merck Index | ||
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6324616
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6998-60-3
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Rifamycin
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DU69T8ZZPA
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CHEMBL437765
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2293
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Related Record | Type | Details | ||
---|---|---|---|---|
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TRANSPORTER -> INHIBITOR |
Rifamycin is an inhibitor of renal transporters organic anion transporter (OAT) 3, multidrug and toxin extrusion (MATE) 1, and MATE2-K transporters in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose, clinically relevant inhibition of these transporters in vivo is unlikely.
|
||
|
METABOLIC ENZYME -> INDUCER |
Rifamycin is an inducer of CYP3A4 and CYP2B6 but not CYP1A2 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose, clinically relevant induction of these enzymes in vivo is unlikely.
|
||
|
TARGET ORGANISM->INHIBITOR | |||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
||
|
TARGET ORGANISM->INHIBITOR |
Other
|
||
|
METABOLIC ENZYME -> INDUCER |
Rifamycin is an inducer of CYP3A4 and CYP2B6 but not CYP1A2 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose, clinically relevant induction of these enzymes in vivo is unlikely.
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR |
Rifamycin is an inhibitor of renal transporters organic anion transporter (OAT) 3, multidrug and toxin extrusion (MATE) 1, and MATE2-K transporters in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose, clinically relevant inhibition of these transporters in vivo is unlikely.
|
||
|
TRANSPORTER -> INHIBITOR |
IC50
|
||
|
TARGET ORGANISM->INHIBITOR | |||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> SUBSTRATE | |||
|
EXCRETED UNCHANGED |
After IV administration of rifamycin SV, > 90% of the dose is excreted as unchanged drug in feces via biliary secretion8
FECAL
|
||
|
SALT/SOLVATE -> PARENT | |||
|
TRANSPORTER -> INHIBITOR |
IC50
|
||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
||
|
METABOLIC ENZYME -> NON-SUBSTRATE | |||
|
TRANSPORTER -> INHIBITOR |
Rifamycin is an inhibitor of renal transporters organic anion transporter (OAT) 3, multidrug and toxin extrusion (MATE) 1, and MATE2-K transporters in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose, clinically relevant inhibition of these transporters in vivo is unlikely.
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
||
|
METABOLIC ENZYME -> INHIBITOR |
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
|
Related Record | Type | Details | ||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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Related Record | Type | Details | ||
---|---|---|---|---|
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ACTIVE MOIETY |