Inocoterone acetate (USAN) (also known as RU-38882, RU-882) is the acetate ester of inocoterone a steroid-like nonsteroidal antiandrogen (NSAA) that was developed for topical administration to treat acne but was never marketed. Inocoterone acetate is actually not a silent antagonist of the androgen receptor but rather a weak partial agonist, similarly to steroidal antiandrogens like cyproterone acetate. In this double-blind study of 126 male subjects with acne, a topical solution of the antiandrogen inocoterone produced a modest but statistically significant reduction in the number of inflammatory acne lesions.

Betamicin is an aminoglycoside antibiotic

Cefaparole (cephaparole) is a cephem antibiotic of the cephalosporin subclass that was never marketed and used as phmarceutical intermediates for other drugs.

Colestolone (5 alpha-cholest-8(14)-en-3 beta-ol-15-one) is an inhibitor of sterol biosynthesis. The compound reduces the level of 3-hydroxy-3-methylglutaryl coenzyme A reductive activity in cultured mammalian cells. In nonhuman primates, the compound decreases the levels of total serum cholesterol and low-density lipoprotein and increases the percentage of total cholesterol associated with high-density lipoprotein.

Metogest, a hormone, is a progesterone receptor agonist. Metogest was used in acne treatment. However, this drug has never been marketed.

Zearalenone (ZEN) is a toxic non-steroidal mycoestrogen produced by fungi that widely contaminate agricultural products, eliciting estrogenic responses by mimicking sex steroid hormones. Zearalenone is biosynthesised through a polyketide pathway by a variety of Fusarium fungi including Fusarium graminearum (Gibberella zeae), Fusarium culmorum, Fusarium equiseti, Fusarium crookwellense, Fusarium cerealis and Fusarium semitectum. Zearalenone and its derivatives share similar molecular mechanisms and activity with estrogens. They interact with the estrogen receptors (ERa and ERb) leading to functional and morphological changes in the reproductive system in both animals and humans. Zearalenone exposure is associated with the estrogenic syndrome and infertility in animals and premature thelarche and precocious puberty in girls. In animal models, it was found that prepubertal exposure to a low dose of Zearalenone, decreased breast cancer risk. When prepubertal rats were treated with 20 lg (1 mg ⁄ kg body weight) of Zearalenone, a significant reduction of both the incidence and multiplicity of DMBA-induced mammary tumours was noted. Zearalenone has been used to treat postmenopausal symptoms in women.

Cocculine is an alkaloid found in the leaves of Cocculus laurifolius, the laurel-leaved snail tree. Cocculine has hypotensive and ganglion blocking properties.

Gloximonam (SQ-82531) is a beta-lactam antibiotic. This is a class of antibiotics that contains a beta-lactam ring in their molecular structure, such as penicillin derivatives. Gloximonam is orally absorbed and has shown anti-bacterial activity against different bacteria of the Enterobacteriaceae and Haemophilus influenzae families. Gloximonam is not effective against staphylococci and strict anaerobes (like aztreonam) and (unlike aztreonam) against Pseudomonas aeruginosa.

Hydroxystenozole is an orally active anabolic-androgenic steroid (AAS) that was described in the literature in 1967 but was never marketed.