Colterol is a beta-2 adrenoreceptor agonist. Bitolterol, a diester prodrug of colterol, was marketed by Elan Pharmaceuticals for the treatment of reversible bronchospasm associated with asthma or chronic obstructive pulmonary diseases.

Moquizone is quinazolinone derivative with choleretic and antifibrillatory activity. Oral toxic doses of Moquizone exerted depressant effects, whereas parenteral toxic doses exerted stimulant effects on the central nervous system.

Metostilenol was developed as an antidepressant. However, it has never been marketed.

Mitoquidone is pentacyclic pyrroloquinone derivative developed for clinical evaluation as a potential anticancer agent. Mitoquidone demonstrated good activity in a range of experimental solid tumour models, but was weakly active against standard prescreens such as the P388 murine leukaemia. Bone marrow suppression or other significant toxicity was not observed in preclinical studies. In clinical trials patients were treated with Mitoquidone given as a 4-h infusion either once every 21 days, once a week, or as 5 daily doses repeated every 28 days. The major adverse events encountered included nausea and vomiting (in virtually all patients), dyspnoea, tumour-related pain, and thrombocytopenia in several patients with pretreatment bone-marrow impairment. Phase I studies were suspended without a maximum tolerated dose being reached because of formulation difficulties. There were no major responses, although stable disease was observed in a number of patients with gastrointestinal malignancies.

Nikkomycin Z is an antifungal drug that inhibits chitin synthase. It has been reported that it inhibits chitin synthases (Chs) 1 and 3, but not 2, of Saccharomyces cerevisiae. Later it was found that nikkomycin Z inhibited all three Chs isozymes of Candida albicans (CaChs). The IC(50) value for CaChs1 is 15 uM, for CaChs2 0.8 uM, and for CaChs3 13 uM. Nikkomycin Z is under development as an orphan product for treatment of coccidioidomycosis. Nikkomycin Z has been used in trials studying the treatment and basic science of Coccidioidomycosis. In February 2006, nikkomycin z was designated as an orphan drug for the treatment of Coccidioidomycosis.

Metamelfalan is an antineoplastic agent. Metamelfalan is the meta form of the levo isomer melphalan. Metamelfalan causes crosslinking of DNA, thereby preventing DNA replication and eventually cellular proliferation.

Nafagrel [DP 1904, SR 96325] is a thromboxane A2 synthetase inhibitor that was undergoing clinical trials with Daiichi Seiyaku, now Daiichi Pharmaceutical, for the diabetic angiopathies, lupus nephritis and Raynaud's disease in Japan. However the development of Nafagrel has been discontinued.

Eticlopride {2S(−)-3-chloro-5-ethyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-hydroxy-2-methoxybenzamide} is an antagonist at dopamine D2 and D3 receptors. It is widely used for in vivo, in vitro, and ex vivo examination of D2/D3 receptors densities and function. Eticlopride exerts antipsychotic activity in animals.

Serfibrate, a clofibrate derivative, is a peroxisome proliferator activated receptor-α (PPAR-α) agonist. It is a hypolipidemic agent.

Glybuthiazole is a sulfonamide derivative with antihyperglycemic activity, which possesses anti-diabetic properties. It is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.