Tetrahydrocannabivarin is a propyl analogue of tetrahydrocannabinol that acts as a Cannabinoid receptor type 1 antagonist and a partial agonist of Cannabinoid receptor type 2. Beyond the endocannabinoid system, Tetrahydrocannabivarin has also been reported to activate 5HT1A receptors to produce an antipsychotic effect that has therapeutic potential for ameliorating some of the negative, cognitive and positive symptoms of schizophrenia. Animal studies have shown that, like rimonabant, Tetrahydrocannabivarin reduces weight gain and food consumption in non-fasted mice but does not increase activity in the brain regions involved in emotion regulation. In another study, involving diet-induced obese mice, oral Tetrahydrocannabivarin reduced body fat content, increased energy expenditure, and reduced fasting insulin and 30-min insulin response to oral glucose tolerance test. In clinical trials THCV significantly decreased fasting plasma glucose and improved pancreatic β-cell function.

Ciprocinonide (RS-2386) is a synthetic glucocorticoid corticosteroid. It was developed in the 1980s for a topical administration as a component of the Triple Corticoid Integrated System.

Procinonide is a derivative of fluocinolone acetonide that has been applied topically with fluocinonide and ciprocinonide in the management of various skin disorders.

Picropodophyllin (also known as picropodophyllotoxin (PPP)), an orally active insulin-like growth factor 1 receptor (IGF1R) inhibitor that exhibits no activity at the insulin receptor, FGFR, PDGFR or EGFR. Picropodophyllin possesses antineoplastic activity. PPP is currently tested as an orally administrated single agent treatment in an open-label combined Phase I/II clinical study in advanced cancer patients with solid tumors which progress in spite of several lines of treatment. In addition, it effectively inhibits rhambodmyosarcomas tumor proliferation and metastasis in vitro and in an animal model.

Fluocinolone participated in clinical trials for the treatment of Oral Lichen Planus and Candida Infection.

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.

16,16-dimethyl Prostaglandin E2 acts as an agonist on most prostaglandin E (EP) receptor subtypes, it has prolonged half-life in vivo, because it is not a substrate for the enzyme 15-hydroxy prostaglandin dehydrogenase. This compound was studied by Fate Therapeutics in phase I clinical trials under the name FT1050 or ProHema-CB for pediatric patients with hematologic malignancies. However, this study was terminated.

Tixanox is an antiallergic drug. It blocks histamine release from human lung induced by anti-IgE. Tixanox has been shown to be orally active against exercise-induced asthma in man.