Creation of a long-acting nanoformulated dolutegravir

Pharmacokinetics of a Long-Acting Nanoformulated Dolutegravir Prodrug in Rhesus Macaques

A nanoformulated myristoylated dolutegravir prodrug (NMDTG) was prepared using good laboratory practice protocols. Intramuscular injection of NMDTG (118 ± 8 mg/ml, 25.5 mg of DTG equivalents/kg of body weight) to three rhesus macaques led to plasma DTG levels of 86 ± 12 and 28 ± 1 ng/ml on days 35 and 91, respectively. The NMDTG platform showed no significant adverse events. Further modificatio...

Creation of a Long-Acting Nanoformulated 2′,3′-Dideoxy-3′-Thiacytidine

BACKGROUND Antiretroviral drug discovery and formulation design will facilitate viral clearance in infectious reservoirs. Although progress has been realized for selected hydrophobic integrase and nonnucleoside reverse transcriptase inhibitors, limited success has been seen to date with hydrophilic nucleosides. To overcome these limitations, hydrophobic long-acting drug nanoparticles were creat...

LONG-ACTING CONTRACEPTIVE AGENTS: TESTOSTERONE ESTERS OF CYCLOALKYLCARBOXYLIC ACIDS

The synthesis of twenty five esters of testosterone (17β -hydroxyandrost- 4-en-3-one) is described. All esters are derivatives of cycloalkycarboxylic acids. Some of the esters possess α- , β -and/or & - substitution in the ester side-chain. The work was undertaken in order to evaluate long-acting male antifertility effect of such esters. Most of the compounds, especially compound No.1, wer...

TREATMENT OF PRECOCIOUS PUBERTY BY A LONG-ACTING GONADOTROPIN-RELEASING HORMONE ANALOGUE IN CHILDREN

The GnRH analogue has been shown to be effective in the treatment of precocious puberty when given as a daily subcutaneous injection. We studied the effectiveness of a long-acting GnRH analogue, Triptoreline, for the treatment of central precocity, by suppressing gonadotropin and estradiol secretion in three children with true precocious puberty. One month after single dose intramuscular i...

Long-acting sulfonylureas -- long-acting hypoglycaemia.