Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C46H62N4O11 |
Molecular Weight | 847.0064 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)CN1CCC2(CC1)N=C3c4c5c(c(C)c6c4C(=O)[C@@](C)(O/C(/[H])=C(\[H])/[C@@]([H])([C@@]([H])(C)[C@]([H])([C@]([H])(C)[C@@]([H])([C@]([H])(C)[C@]([H])([C@@]([H])(C)/C(/[H])=C(\[H])/C(/[H])=C(/C)\C(=NC(=C3N2)C5=O)O)O)O)OC(=O)C)OC)O6)O
InChI
InChIKey=ATEBXHFBFRCZMA-VXTBVIBXSA-N
InChI=1S/C46H62N4O11/c1-22(2)21-50-18-16-46(17-19-50)48-34-31-32-39(54)28(8)42-33(31)43(56)45(10,61-42)59-20-15-30(58-11)25(5)41(60-29(9)51)27(7)38(53)26(6)37(52)23(3)13-12-14-24(4)44(57)47-36(40(32)55)35(34)49-46/h12-15,20,22-23,25-27,30,37-38,41,49,52-54H,16-19,21H2,1-11H3,(H,47,57)/b13-12+,20-15+,24-14-/t23-,25+,26+,27+,30-,37-,38+,41+,45-/m0/s1
Molecular Formula | C46H62N4O11 |
Molecular Weight | 847.0064 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment:: description was created based on several sources, including:
https://www.drugs.com/cdi/rifabutin.html
http://www.rxlist.com/mycobutin-drug.htm
http://www.wikidoc.org/index.php/Rifabutin
Curator's Comment:: description was created based on several sources, including:
https://www.drugs.com/cdi/rifabutin.html
http://www.rxlist.com/mycobutin-drug.htm
http://www.wikidoc.org/index.php/Rifabutin
Rifabutin 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 aeruginosa) and specifically Mycobacterium tuberculosis. It is FDA approved for the prophylaxis of disseminated Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection. Multiple dosing of rifabutin has been associated with induction of hepatic metabolic enzymes of the CYP3A subfamily. Rifabutin’s predominant metabolite (25-desacetyl rifabutin: LM565), may also contribute to this effect. Similarly, concomitant medications that competitively inhibit the CYP3A activity may increase plasma concentrations of rifabutin. Common adverse reactions include discoloration of skin, rash, diarrhea, disorder of taste, indigestion, loss of appetite, nausea, vomiting, increased liver aminotransferase level (mild), ocular discoloration, uveitis, abnormal color of body fluid.
CNS Activity
Sources: http://img.thebody.com/nih/prof/rifabutin.pdf
Curator's Comment:: Because of frequent side effects at high doses (e.g., arthralgia, uveitis, and stomatitis), rifabutin has rarely been used to treat CNS infections.
https://www.ncbi.nlm.nih.gov/pubmed/20930076
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL340 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18713760 |
|||
Target ID: P0A8V2 Gene ID: 948488.0 Gene Symbol: rpoB Target Organism: Escherichia coli (strain K12) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | MYCOBUTIN Approved UseMYCOBUTIN Capsules are indicated for the prevention of disseminated Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection. Launch Date7.2506881E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
613 ng/mL |
450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
691 ng/mL |
450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5803 ng × h/mL |
450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
9287 ng × h/mL |
450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
58 h |
450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
45 h |
450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
21.5% |
450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered: |
RIFABUTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Other AEs: Abdominal pain, Asthenia... Other AEs: Abdominal pain (4%) Sources: Asthenia (1%) Chest pain (1%) Fever (2%) Headache (3%) Pain (1%) Anorexia (2%) Diarrhea (3%) Dyspepsia (3%) Eructation (3%) Flatulence (2%) Nausea (6%) Nausea and vomiting (3%) Vomiting (1%) Myalgia (2%) Insomnia (1%) Rash (11%) Taste perversion (3%) Urine discoloration (30%) Alkaline phosphatase increased (<1%) SGOT increased (7%) SGPT increased (9%) Anemia (6%) Eosinophilia (1%) Leukopenia (17%) Neutropenia (25%) Thrombocytopenia (5%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Asthenia | 1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Chest pain | 1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Eosinophilia | 1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Insomnia | 1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Pain | 1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Vomiting | 1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Rash | 11% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Leukopenia | 17% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Anorexia | 2% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Fever | 2% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Flatulence | 2% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Myalgia | 2% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Neutropenia | 25% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Diarrhea | 3% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Dyspepsia | 3% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Eructation | 3% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Headache | 3% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Nausea and vomiting | 3% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Taste perversion | 3% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Urine discoloration | 30% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Abdominal pain | 4% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Thrombocytopenia | 5% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Anemia | 6% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Nausea | 6% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
SGOT increased | 7% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
SGPT increased | 9% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Alkaline phosphatase increased | <1% | 300 mg 1 times / day multiple, oral Recommended Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: |
unhealthy, adult n = 566 Health Status: unhealthy Condition: Mycobacterium avium complex (MAC) disease in patients with advanced HIV infection Age Group: adult Population Size: 566 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
likely | ||||
no | ||||
no | ||||
no | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/24060875/ |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/24060875/ |
no | |||
no | ||||
no | ||||
unlikely [IC50 31.5 uM] | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/24060875/ |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/24060875/ |
yes | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/24060875/ |
yes | |||
yes | yes (co-administration study) Comment: many DDIs: see https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/050689s016lbl.pdf#page=3 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
yes | ||||
yes |
PubMed
Title | Date | PubMed |
---|---|---|
Biological activity of a new class of rifamycins. Spiro-piperidyl-rifamycins. | 1980 Oct |
|
In vitro susceptibility of Mycobacterium avium complex and Mycobacterium tuberculosis strains to a spiro-piperidyl rifamycin. | 1982 Sep |
|
Activity of the spiropiperidyl rifamycin LM 427 on rifampicin resistant Mycobacterium tuberculosis. | 1984 Sep-Dec |
|
Determination of ansamycin MICs for Mycobacterium avium complex in liquid medium by radiometric and conventional methods. | 1985 Oct |
|
Comparative in vitro activities of MDL 473, rifampin, and ansamycin against Mycobacterium intracellulare. | 1985 Sep |
|
Determination of in vitro susceptibility of mycobacteria to ansamycin. | 1985 Sep |
|
Determination of MICs of conventional and experimental drugs in liquid medium by the radiometric method against Mycobacterium avium complex. | 1987 |
|
Activity of rifabutin alone or in combination with clofazimine or ethambutol or both against acute and chronic experimental Mycobacterium intracellulare infections. | 1987 Aug |
|
In vitro susceptibility of Mycobacterium avium complex to antibacterial agents. | 1987 Nov |
|
Action of antituberculous and beta-lactam drugs (including imipenem) against extra- and intra-cellularly growing Mycobacterium avium-intracellulare. | 1988 Mar-Apr |
|
Interaction between rifabutin and human immunodeficiency virus type 1: inhibition of replication, cytopathic effect, and reverse transcriptase in vitro. | 1988 May |
|
Comparative in vitro and in vivo activity of rifabutin and rifampicin against Mycobacterium avium complex. | 1988 Sep |
|
In vitro activities against mycobacteria of two long-acting rifamycins, FCE22807 and CGP40/469A (SPA-S-565). | 1990 Jun |
|
Effect of rifabutin on disseminated Mycobacterium avium infections in thymectomized, CD4 T-cell-deficient mice. | 1990 Sep |
|
[In vivo activities of new rifamycin derivatives against mycobacteria]. | 1991 Jan |
|
In vitro antimycobacterial activities of newly synthesized benzoxazinorifamycins. | 1991 Mar |
|
Oxazolidinones, a new class of synthetic antituberculosis agent. In vitro and in vivo activities of DuP-721 against Mycobacterium tuberculosis. | 1991 Nov-Dec |
|
Effectiveness of rifampin, rifabutin, and rifapentine for preventive therapy of tuberculosis in mice. | 1993 Dec |
|
Azithromycin, rifabutin, and rifapentine for treatment and prophylaxis of Mycobacterium avium complex in rats treated with cyclosporine. | 1993 Mar |
|
Anti-Mycobacterium avium activity of quinolones: in vitro activities. | 1993 Sep |
|
Rifabutin is active in murine models of toxoplasmosis. | 1994 Mar |
|
In vitro and in vivo antibacterial activities of KRM-1648 and KRM-1657, new rifamycin derivatives. | 1994 May |
|
A bone marrow-derived murine macrophage model for evaluating efficacy of antimycobacterial drugs under relevant physiological conditions. | 1994 Nov |
|
Effectiveness of various antimicrobial agents against Mycobacterium avium complex in the beige mouse model. | 1994 Nov |
|
Clinical experience with rifabutin in the treatment of mycobacterial infections. | 1995 |
|
[Extra and intracellular activity of dirithromycin against Mycobacterium avium]. | 1995 Apr |
|
In-vitro and intracellular activity of rifabutin on drug-susceptible and multiple drug-resistant (MDR) tubercle bacilli. | 1995 Aug |
|
Mutation position and type of substitution in the beta-subunit of the RNA polymerase influence in-vitro activity of rifamycins in rifampicin-resistant Mycobacterium tuberculosis. | 1995 Feb |
|
Activities of rifabutin, clarithromycin, and ethambutol against two virulent strains of Mycobacterium avium in a mouse model. | 1995 Mar |
|
Comparison of activities of fluoroquinolones in murine macrophages infected with Mycobacterium tuberculosis. | 1995 Mar |
|
In vitro and in vivo activities of the benzoxazinorifamycin KRM-1648 against Mycobacterium tuberculosis. | 1995 Oct |
|
Activity of seven antimicrobial agents, alone and in combination, against AIDS-associated isolates of Mycobacterium avium complex. | 1995 Sep |
|
New drugs for tuberculosis. | 1995 Sep |
|
Chemotherapeutic activity of benzoxazinorifamycin, KRM-1648, against Mycobacterium tuberculosis in C57BL/6 mice. | 1996 Apr |
|
Susceptibility testing of Mycobacterium avium complex isolates. | 1996 Aug |
|
How effective is KRM-1648 in treatment of disseminated Mycobacterium avium complex infections in beige mice? | 1996 Feb |
|
Rifamycin resistance in mycobacteria. | 1996 Jan-Feb |
|
Rifapentine is active in vitro and in vivo against Toxoplasma gondii. | 1996 Jun |
|
Activity of rifabutin, clarithromycin, ethambutol, sparfloxacin and amikacin, alone and in combination, against Mycobacterium avium complex in human macrophages. | 1996 Mar |
|
Use of rifabutin in combination with atovaquone, clindamycin, pyrimethamine, or sulfadiazine for treatment of toxoplasmic encephalitis in mice. | 1996 May |
|
Evaluation of the activities of rifabutin combined with atovaquone or low-dose of cotrimoxazole for prevention of pneumocystosis and toxoplasmosis in a dual infection rat model. | 1996 Sep-Oct |
|
Rapid drug susceptibility of Mycobacterium avium complex using a fluorescence quenching method. | 1997 Aug |
|
Clinically used antimicrobial drugs against experimental pneumocystosis, singly and in combination: analysis of drug interactions and efficacies. | 1997 Feb |
|
[Therapeutic efficacy of benzoxazinorifamycin KRM-1648 against experimental murine tuberculosis: (1). A study on the efficacy of short course treatment with the intratracheal and intravenous infection model]. | 1998 Feb |
|
Contribution of rpoB mutations to development of rifamycin cross-resistance in Mycobacterium tuberculosis. | 1998 Jul |
|
Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction. | 2006 Oct |
|
Efficacy of rifabutin-loaded microspheres for treatment of Mycobacterium avium-infected macrophages and mice. | 2007 Mar |
|
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. | 2010 Dec |
|
Human arylacetamide deacetylase is responsible for deacetylation of rifamycins: rifampicin, rifabutin, and rifapentine. | 2011 Dec 1 |
|
The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment. | 2012 Sep 15 |
Patents
Sample Use Guides
It is recommended that Rifabutin Capsules be administered at a dose of 300 mg once daily. For those patients with propensity to nausea, vomiting, or other gastrointestinal upset, administration of Rifabutin at doses of 150 mg twice daily taken with food may be useful.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7706160
The IC50 of rifabutin was 26.5 mg/L in a different series of experiments using an enzyme-linked immunoassay and the T. gondii high virulence strain.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 21:05:16 UTC 2021
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admin
on
Fri Jun 25 21:05:16 UTC 2021
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Record UNII |
1W306TDA6S
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Record Status |
Validated (UNII)
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Record Version |
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-
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QJ04AB04
Created by
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NCI_THESAURUS |
C280
Created by
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NDF-RT |
N0000007911
Created by
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LIVERTOX |
844
Created by
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NDF-RT |
N0000007911
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admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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NDF-RT |
N0000007911
Created by
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NDF-RT |
N0000007911
Created by
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FDA ORPHAN DRUG |
41989
Created by
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WHO-ATC |
J04AB04
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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FDA ORPHAN DRUG |
770820
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NDF-RT |
N0000175501
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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WHO-ESSENTIAL MEDICINES LIST |
6.2.4
Created by
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FDA ORPHAN DRUG |
338811
Created by
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FDA ORPHAN DRUG |
41889
Created by
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Code System | Code | Type | Description | ||
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Rifabutin
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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RIFABUTIN
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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5668
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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M9608
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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PRIMARY | Merck Index | ||
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6323490
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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55672
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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PRIMARY | RxNorm | ||
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2376
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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C1408
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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D017828
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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72559-06-9
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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SUB10304MIG
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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1W306TDA6S
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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1603800
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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PRIMARY | USP-RS | ||
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DB00615
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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3577
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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72559-06-9
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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CHEMBL444633
Created by
admin on Fri Jun 25 21:05:16 UTC 2021 , Edited by admin on Fri Jun 25 21:05:16 UTC 2021
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> INDUCER | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> INDUCER |
Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PARENT |
MAJOR
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
MAJOR
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (TLC)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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Related Record | Type | Details | ||
---|---|---|---|---|
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ACTIVE MOIETY |