Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI) and INSTIs are the latest class of potent anti-HIV drugs.Compared to the first generation INSTIs, raltegravir, and elvitegravir, Dolutegravir shows a limited cross-resistance profile.More interestingly, clinical resistance mutations to Dolutegravir in treatment-naive patents have not been observed to this date.Dolutegravir is a dominant strategy in the management of TN and TE patients when compared to recommended comparators.Dolutegravir had no effect on NGM/EE PK or PD. NGM/EE can be administered with DTG without dose adjustment.Dolutegravir is the integrase inhibitor of choice for rescue therapy in multiresistant HIV infection, both in integrase inhibitor-naïve patients and in those previously treated with raltegravir or elvitegravir.Treatment with DTG led to less HIV-1 genetic and amino-acid diversification over time, as compared to treatment with RAL or the absence of drug.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO >4 mg/ml|
Cost-Effectiveness of Dolutegravir in HIV-1 Treatment-Naive and Treatment-Experienced Patients in Canada.
Despiégel N, et al. Infect Dis Ther. 2015 Jun 23. PMID: 26099626.
Will drug resistance against dolutegravir in initial therapy ever occur?
Wainberg MA, et al. Front Pharmacol. 2015 Apr 29;6:90. PMID: 25972810.
Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol.
Song IH, et al. Ann Pharmacother. 2015 Jul;49(7):784-9. PMID: 25862012.
[Efficacy of dolutegravir in treatment-experienced patients: the SAILING and VIKING trials].
Moreno S, et al. Enferm Infecc Microbiol Clin. 2015 Mar;33 Suppl 1:26-30. PMID: 25858609.
Dolutegravir inhibits HIV-1 Env evolution in primary human cells.
Mesplède T, et al. AIDS. 2015 Mar 27;29(6):659-65. PMID: 25849829.
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|Apelin-36(rat, mouse) TFA
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist.
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