The present invention is generally directed to a method of increasing testosterone levels in a subject comprising administration of testosterone or analogue thereof along with an ornithine decarboxylase (ODC) inhibitor. The method selectively promotes beneficial effects of testosterone, while preventing side effects associated with testosterone administration. The present invention also directed to pharmaceutical composition and kits comprising testosterone or analogue thereof ornithine decarboxylase inhibitors. The composition selectively promotes beneficial effects of testosterone, while preventing side effects of testosterone administration. In some embodiments, the present invention relates to a method of treatment of low testosterone levels in a subject by administrating testosterone and ODC inhibitor while preventing side effects associated with testosterone administration. The method and composition of the invention particularly prevents potential adverse effects on the prostate in men and virilization in women.