Dolutegravir (Tivicay) was a new kind of anti-ADIS drug that jointly developed by the British pharmaceutical giant GlaxoSmithKline (GSK) with the Japanese Shionogi Pharmaceutical Company (Shionogi).
In July 2012, the GlaxoSmithKline Pharmaceuticals and Japan's Shionogi Pharmaceutical Company announced the results of Phase III clinical trial of the new AIDS drug Dolutegravir. After 48 weeks of treatment with dolutegravir and two other older versions of the AIDS drug, 88% of the virus in vivo was successfully inhibited, while the use of Gilead Sciences (Gilead Sciences) of the three-in-one oral drug Atripla (Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate), 81% of the virus in patients was inhibited, which can be seen that, the dolutegravir developed by the GlaxoSmithKline pharmaceutical companies is slightly better. According to the researchers, in a comparative trial, owing to the side effects of the drugs, 10% of the patients stopped taking the Atripla drug developed from Gilead Technologies while only 2% stopped taking GlaxoSmithKline's dolutegravir Drug, therefore, we can see that the dolutegravir drugs from GlaxoSmithKline has slightly higher safety.
On August 12, 2013, the US Food and Drug Administration (FDA) approved the use of dolutegravir for being used in previously treated or early treated HIV-1 adults and 12 years of age and above infected children of at least 40 kg.
Dolutegravir is a once-daily drug with its efficacy being comparable to Merck's HIV/AIDS drug Raltegravir (Isentress) in Phase III clinical trials. Raltegravir should be subject to daily administration twice. Both of them are inhibitors of HIV integrase. The FDA official claim that the AIDS patient should be subject to targeted treatment on a case-by-case basis. Tivicay will provide patients with new options. In a study done a year ago, 88% of patients had a significant improvement after 48 weeks of Tivicay treatment, better than the efficacy of the Gilead's Atripla. Analysts expect that Dolutegravir will become a multi-billion-dollar blockbuster drug and a strong contender for Atripla, the world's best-selling HIV drug, developed by Gilead Sciences.
Common name: Dolutegravir
Trade name: Tivicay
Alias: GSK1349572, S-349572, GSK572
Drug Company: GlaxoSmithKline
Drug type: integrase inhibitors
Approved date: August 12, 2013 (US)
CAS Registry Number: 1051375-16-6
Chemical name: (4R, 12aS)-N-[(2, 4-difluorophenyl) methyl]-3, 4, 6, 8, 12, 12a-hexahydro-7-hydroxy-Dioxo-2H-pyrido [1 ', 2': 4,5] pyrazino [2,1-b] [1,3] oxazine-9-carboxamide
U.S. Patent No. 8,129,385
The patent expires on October 5, 2027
International patent: W02006116764
This information is compiled and edited by Xiao Nan of Chemicalbook.
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 peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
Dolutegravir (GSK1349572) is a HIV integrase inhibitor with an IC50 of 2.7 nM and is moderately effective against the significant mutants Y143R, Q148K, N155H, and G140S/Q148H against Raltegravir.
ChEBI: 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]ox
zine-9-carboxylic acid with the amino group of 2,4-difluorobenzylamine. Used (as its sodium salt) for treatment of HIV-1.