CAS No. : 1051375-16-6

Product Details
Cat No:A000782
Synonyms:GSK1349572;GSK 1349572
Molecular Formula:C₂₀H₁₉F₂N₃O₅
Molecular Weight:419.38
Target:HIV Integrase
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Appearance: Solid powder
Purity: > 98%
Cat No:A000782
Cas No:1051375-16-6

Dolutegravir(CAS 1051375-16-6), also known as GSK1349572, is an FDA-approved drug for the treatment of HIV infection. 

Dolutegravir can be used to treat HIV-infected adults who have never taken HIV therapy (treatment-naïve) and HIV-infected adults who have previously taken HIV therapy (treatment-experienced), including those who have been treated with other integrase strand transfer inhibitors. Tivicay is also approved for children ages 12 years and older weighing at least 40 kilograms (kg) who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors.

1. AIDS. 2010 Nov 13;24(17):2753-5. doi: 10.1097/QAD.0b013e32833f9e36.
In-vitro phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitor S/GSK1349572.
Charpentier C(1), Larrouy L, Collin G, Damond F, Matheron S, Chêne G, Nie T, Schinazi R, Brun-Vézinet F, Descamps D; French ANRS HIV-2 Cohort (ANRS CO 05 VIH-2).
Author information:
(1)Assistance Publique-Hôpitaux de Paris, Hôpital Bichat-Claude Bernard, Université Paris-Diderot, France.
In this study of nine clinical isolates obtained from integrase inhibitor-naïve HIV-2-infected patients, the median EC₅₀ value for the new integrase inhibitor S/GSK1349572 was 0.8 nM (range 0.2-1.4), and is similar to HIV-1 reference strains. We found a seven-, 13- and 18-fold increase in EC₅₀ values to S/GSK1349572 for the HIV-2 double (T97A + Y143C; G140S + Q148R) and triple (G140T + Q148R + N155H) mutants, respectively, obtained from two raltegravir-experienced patients.

2. J Acquir Immune Defic Syndr. 2010 Nov;55(3):365-7. doi: 10.1097/QAI.0b013e3181e67909.
Lack of interaction between the HIV integrase inhibitor S/GSK1349572 and tenofovir in healthy subjects.
Song I(1), Min SS, Borland J, Lou Y, Chen S, Ishibashi T, Wajima T, Piscitelli SC.
Author information:
(1)GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
BACKGROUND: The potential for a drug interaction between S/GSK1349572 and tenofovir disoproxil fumarate (TDF) was evaluated in an open-label, repeat dose, 3-period, drug-drug interaction study in healthy subjects.
METHODS: S/GSK1349572 was administered at 50 mg once daily for 5 days (period 1) followed by a 6-day washout period. TDF 300 mg once daily was then administered for 7 days (period 2). The combination of S/GSK1349572 and TDF was then coadministered for 5 days (period 3). Pharmacokinetic parameters were determined and compared between periods.
RESULTS: Fifteen subjects completed all periods and follow-up. S/GSK1349572 and TDF were generally well tolerated with few adverse events reported. No clinically significant trends in post-dose laboratory abnormalities, vital signs, or electrocardiogram values were noted. Pharmacokinetic parameters of S/GSK1349572 and tenofovir during combination therapy were similar to those when given alone, demonstrating no significant drug interaction. S/GSK1349572 geometric least squares mean ratios (90% confidence interval) for AUC(0-τ), Cmax, and Cτ were 1.01 (0.908, 1.11), 0.969 (0.867, 1.08), and 0.920 (0.816, 1.04), respectively. Tenofovir geometric least squares mean ratios (90% confidence interval) for AUC(0-τ), Cmax, and Cτ were 1.12 (1.01, 1.24), 1.09 (0.974, 1.23), and 1.19 (1.04, 1.35), respectively.
CONCLUSION: S/GSK1349572 and TDF can be coadministered without dose adjustment.

3. Antimicrob Agents Chemother. 2010 Jan;54(1):254-8. doi: 10.1128/AAC.00842-09. Epub 2009 Nov 2.
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.
Min S(1), Song I, Borland J, Chen S, Lou Y, Fujiwara T, Piscitelli SC.
Author information:
(1)Infectious Diseases MDC, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA.
S/GSK1349572 is a novel integrase inhibitor with potent in vitro anti-HIV activity, an in vitro resistance profile different from those of other integrase inhibitors, and favorable preclinical safety and pharmacokinetics (PK). Randomized, double-blind, placebo-controlled single-dose and multiple-dose, dose escalation studies evaluated the PK, safety, and tolerability of S/GSK1349572 for healthy subjects. In the single-dose study, two cohorts of 10 subjects each (8 active, 2 receiving placebo) received suspension doses of 2, 5, 10, 25, 50, and 100 mg in an alternating panel design. In the multiple-dose study, three cohorts of 10 subjects each (8 active, 2 receiving placebo) received suspension doses of 10, 25, and 50 mg once daily for 10 days. A cytochrome P450 3A (CYP3A) substudy with midazolam was conducted with the 25-mg dose. Laboratory testing, vital signs, electrocardiograms (ECGs), and PK sampling were performed at regular intervals. S/GSK1349572 was well tolerated. Most adverse events (AEs) were mild, with a few moderate AEs reported. Headache was the most common AE. No clinically significant laboratory trends or ECG changes were noted. PK was linear over the dosage range studied. The steady-state geometric mean area under the concentration-time curve over a dosing interval (AUC(0-tau)) and maximum concentration of the drug in plasma (C(max)) ranged from 16.7 microg.h/ml (coefficient of variation [CV], 15%) and 1.5 microg/ml (CV, 24%) at a 10-mg dose to 76.8 microg.h/ml (CV, 19%) and 6.2 microg/ml (CV, 15%) at a 50-mg dose, respectively. The geometric mean steady-state concentration at the end of the dosing interval (C(tau)) with a 50-mg dose was 1.6 microg/ml, approximately 25-fold higher than the protein-adjusted 90% inhibitory concentration (0.064 microg/ml). The half-life was approximately 15 h. S/GSK1349572 had no impact on midazolam exposure, indicating that it does not modulate CYP3A activity. The PK profile suggests that once-daily, low milligram doses will achieve therapeutic concentrations.
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