Dolutegravir Approved by the FDA as an Effectual Integrase Inhibitor


Dolutegravir CAS 1051375-16-6On August 12, 2013 Viiv Healthcare proudly announced the FDA approval of the integrase inhibitor, Dolutegravir to combat the HIV virus. Known as the brand name Tivicay, Dolutegravir is typically used in combination with other antiretroviral medications to treat patients with AIDS, ages twelve and older. With many patients living longer while being infected with the HIV virus there are growing concerns over the lack of new treatment options for this patient population. The approval of Dolutegravir offers a novel and versatile treatment option for patients with AIDS who have had a lack of success with their current prescription regimen, and for patients who wish to try medications that may offer fewer adverse side effects.

Results gleaned from four clinical trials, which encompassed 2,557 adults, offered solid proof that treatment with Dolutegravir was not only effective, but also allowed physicians to better individualize patient dosing. The Phase III clinical trials revealed the bulk of the positive news regarding Dolutegravir, and showcased the unique ability of this new drug to elicit fewer negative side effects when compared to other similar medications. One such study, coined “SAILING”, compared a once a day dose of Dolutegravir with a twice daily dose of Raltegravir in patients who were currently faltering on current standard therapy for the HIV infection. Of the 719 adult patients enrolled in this particular study not one had previously received treatment involving an integrase inhibitor, such as Dolutegravir. By the twenty-fourth week of the “SAILING” study almost eighty (80) percent of patients were labeled as virologically suppressed after treatment with Dolutegravir, showing an HIV-1 RNA of less than 50 c/mL. The patients who received Raltegravir also demonstrated success, but at a lesser rate, with seventy (70) percent of these patients experiencing virologic suppression. Dolutegravir proved to be safe and tolerable as well, with no recorded severe adverse reactions leading patients to withdraw from the study.

The “VIKING-3” study of Dolutegravir was another significant Phase III study that offered distinctly encouraging results from HIV positive patients who received consistent treatment with this drug.  Dolutegravir (Tivicay) was dispensed to 183 adults with drug resistant cases of AIDS in the “VIKING-3” study, with a caveat of drug resistance from all patients involved. The patients were all resistant to former integrase inhibitors, including Raltegravir and Elvitegravir, presenting quite a challenge. However, treatment with Dolutegravir showed an average level of HIV RNA decline by 1.4 log10 c/mL after only seven days of treatment. The addition of Dolutegravir to the current cocktail of AIDS medications offered this specific group of HIV positive patients hope and encouragement.

Side effects of Dolutegravir were not reported by clinical trial participants to be severe, with most patients complaining of insomnia and headaches. It is important to note that patients who receive Dolutegravir should not be co-administered the anti-arrhythmic drug dofetilide, due to the risk of life threatening effects.  Dolutegravir is available in 50 milligram tablets, and the usual adult dosage is 50 milligrams twice a day.

LGM Pharma provides API Dolutegravir, CAS number 1051375-16-6, for research and development purposes. Clients can be assured of continuous support throughout the R&D process, as well as quality API products.

 

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