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Dolutegravir



Chemical Properties of 'Dolutegravir'

CAT No. :

CS-O-00218
CAS Registry No. : 1051375-16-6
Category : API Standards
Molecular Weight: 419.38
Molecular Formula : C₂₀H₁₉F₂N₃O₅
Controlled Substance : NO
Documents:  View Sample COA   View Sample MSDS



OTHER INFORMATION of 'Dolutegravir'
Purity : Not less than 95%
Therapeutic : Antiretroviral / Anti-HIV
Applicationnotes :Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peri
Synonym :Not available
References :"Kobayashi; M, et al, Antimcrob Agentschemother,; 55; 813 (2011); Garrido;c, et al,: Antiviral; Res,; 90; 164 (2011); Lenz; Jcc, et al,: Exp, Opin, Invest, Drugs; 20; 537 (2011);"
Smileys :CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
Appearance :White to off white solid
EC Number :809-888-1
UNII :DKO1W9H7M1
NCI Thesaurus Code :C121543
RXCUI :1433868
MeSH Entry Terms :(4R,12aS)-N-((2,4-difluorophenyl)methyl)-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2H-Pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9-carboxamide
Other Synonyms :Dolutegravir
Removed Synonyms :Cabotegravir
CompoundIs Canonicalized :Yes
Vapor Pressure : 1.39X10-17 mm Hg at 25 °C (est)
Other Experimental Properties :White to light yellow powder; slightly soluble in water /Dolutegravir sodium/
GHS Classification :
Toxicity Summary :There was no significant increases in drug-related neoplasms or in genotoxic effects or in mating or fertility effects.
Hepatotoxicity :In large clinical trials, therapy with dolutegravir was associated with alanine aminotransferase (ALT) elevations of greater than 3 times the upper limit of normal (ULN) in 2% to 5% of patients, but these rates were similar to those in comparator groups receiving matched background optimized antiretroviral therapy without dolutegravir. These elevations were not associated with clinical symptoms and generally did not require dose modification. A few instances of acute liver injury with jaundice were described in the registration trials for dolutegravir which occurred in association with hypersensitivity reactions and resolved with drug discontinuation. The clinical features of these cases were not provided and their association with dolutegravir as opposed to the concurrent antiretroviral agents was not fully established. Since its approval and more wide spread use, however, several case reports of acute hepatitis attributable to dolutegravir have appeared. The latency to onset varried from 1 to 8 months and the pattern of serum enzyme elevations was hepatocellular. Immunoallergic and autoimmune features were not present. At least one published case resulted in acute liver failure and need for liver transplanation. The product label for dolutegravir mentions hepatitis and hepatic failure as potential adverse reactions and states that patients with hepatitis B or C coinfection are susceptible to worsening or flares of hepatitis with initiation of dolutegravir therapy, perhaps as a consequence of immune reconstitution syndrome. Monitoring of liver tests is recommended in patients starting regimens that include dolutegravir.
Interactions :Dolutegravir is metabolized by UGT1A1 with some contribution from CYP3A. Dolutegravir is also a substrate of UGT1A3, UGT1A9, BCRP, and P-gp in vitro. Drugs that induce those enzymes and transporters may decrease dolutegravir plasma concentration and reduce the therapeutic effect of dolutegravir. Coadministration of dolutegravir and other drugs that inhibit these enzymes may increase dolutegravir plasma concentration. Etravirine significantly reduced plasma concentrations of dolutegravir, but the effect of etravirine was mitigated by coadministration of lopinavir/ritonavir or darunavir/ritonavir, and is expected to be mitigated by atazanavir/ritonavir. Darunavir/ritonavir, lopinavir/ritonavir, rilpivirine, tenofovir, boceprevir, telaprevir, prednisone, rifabutin, and omeprazole had no clinically significant effect on the pharmacokinetics of dolutegravir.
Antidoteand Emergency Treatment :/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
Human Toxicity Excerpts :/HUMAN EXPOSURE STUDIES/ Dolutegravir is primarily metabolized and eliminated by the liver. In a trial comparing 8 subjects with moderate hepatic impairment (Child-Pugh Score B) with 8 matched healthy controls, exposure of dolutegravir from a single 50-mg dose was similar between the 2 groups. No dosage adjustment is necessary for patients with mild to moderate hepatic impairment (Child-Pugh Score A or B). The effect of severe hepatic impairment (Child-Pugh Score C) on the pharmacokinetics of dolutegravir has not been studied. Therefore, TIVICAY is not recommended for use in patients with severe hepatic impairment.
Non Human Toxicity Excerpts :/LABORATORY ANIMALS: Chronic Exposure or Carcinogenicity/ Two-year carcinogenicity studies in mice and rats were conducted with dolutegravir. Mice were administered doses of up to 500 mg/kg, and rats were administered doses of up to 50 mg/kg. In mice, no significant increases in the incidence of drug-related neoplasms were observed at the highest doses tested, resulting in dolutegravir AUC exposures approximately 14-fold higher than those in humans at the recommended dose of 50 mg twice daily. In rats, no increases in the incidence of drug-related neoplasms were observed at the highest dose tested, resulting in dolutegravir AUC exposures 10-fold and 15-fold higher in males and females, respectively, than those in human at the recommended dose of 50 mg twice daily.
Protein Binding :Dolutegravir is highly protein bound to human plasma proteins reaching a percentage 98.9% of the administered dose.
Exact Mass :419.12927704
IUPAC Name :(3S,7R)-N-[(2,4-difluorophenyl)methyl]-11-hydroxy-7-methyl-9,12-dioxo-4-oxa-1,8-diazatricyclo[8.4.0.03,8]tetradeca-10,13-diene-13-carboxamide
InChI :InChI=1S/C20H19F2N3O5/c1-10-4-5-30-15-9-24-8-13(17(26)18(27)16(24)20(29)25(10)15)19(28)23-7-11-2-3-12(21)6-14(11)22/h2-3,6,8,10,15,27H,4-5,7,9H2,1H3,(H,23,28)/t10-,15+/m1/s1
InchIKey :RHWKPHLQXYSBKR-BMIGLBTASA-N
Canonical SMILES :CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
Isomeric SMILES :C[C@@H]1CCO[C@@H]2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
Melting Point :190-193ºC
Solubility :Slightly soluble
Use Classification :Human drugs -> Tivicay -> EMA Drug Category
Hazard Class :Aquatic Acute 1 (100%)
Product Description :Dolutegravir is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (4R,12aS)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid with the amino group of 2,4-difluorobenzylamine. Used (as its sodium salt) for treatment of HIV-1. It has a role as a HIV-1 integrase inhibitor. It is a monocarboxylic acid amide, an organic heterotricyclic compound, a secondary carboxamide and a difluorobenzene. It is a conjugate acid of a dolutegravir(1-).
Custom Duty : Applicable
Port of Loading : Canada
Expected Dispatch : 14-Aug-2022
Taxes : Not Applicable
Refund Policy : 30-days money back


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What is Dolutegravir ?
Dolutegravir falls under API Standards of Dolutegravir.Dolutegravir is a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir is currently in Phase III clinical trials for the treatment of HIV infection. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peri
What is the CAS Number of Dolutegravir?
The CAS Number of Dolutegravir is 1051375-16-6
Who are the suppliers of Dolutegravir?
CLEARSYNTH is a worldwide supplier of Dolutegravir

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