A phase III, single-arm, 6-month trial of a wide-dose range oral testosterone undecanoate product.

Background: Oral testosterone undecanoate (TU) formulations may provide effective, safe, and easily titratable testosterone replacement therapy.

Objective: Demonstrate efficacy and safety of a novel oral TU formulation.

Design: An open-label, single-arm, multi-center trial treated 155 hypogonadal men for 180 days.

Effects of the oral testosterone undecanoate Kyzatrex™ on ambulatory blood pressure in hypogonadal men.

Testosterone replacement therapies have been shown to increase blood pressure (BP) in hypogonadal men. We studied the effects of a new formulation of testosterone undecanoate (Kyzatrex™) on ambulatory blood pressure (ABP) and heart rate, in 155 men with hypogonadism (mean age, 50.5 years, 76.

Importance of measuring testosterone in enzyme-inhibited plasma for oral testosterone undecanoate androgen replacement therapy clinical trials.

Aim: Testosterone undecanoate (TU) is metabolized by nonspecific esterases in blood to testosterone (T). Typical clinical practice has been to analyze testosterone in human serum. The degradation of TU to testosterone was evaluated in conditions typically used in clinical studies.

Total synthesis of macrodiolide ionophores aplasmomycin A and boromycin via double ring contraction.

The half structure of the symmetrical macrodiolide aplasmomycin A was synthesized by alkylation of a C3-C10 α-sulfonyl ketone subunit, prepared from (R)-pulegone and protected as a C3 ortholactone with (2R,3R)-butanediol, by a protected 15,16-dihydroxy (12E)-allylic chloride representing C11-C17. The latter was obtained from (2S,3R)-1,2-epoxy-3-butanol and propargyl alcohol. Regio- and stereoselective 5-exo-trig cyclization of the ene diol moiety in this segment, mediated by N-bromosuccinimide, led to the (2R,3S,5R)-tetrahydrofuran substructure of aplasmomycin A.