Cefmepidium is a semisynthetic cephalosporin with broad antibacterial activity against penicillin-resistant strains.

Atigliflozin (also known as AVE2268), a substituted glycopyranoside, is a selective inhibitor of sodium-dependent glucose transporter 2. This drug reached phase II clinical trials as a new antidiabetic drug for the treatment of type 2 diabetes but further development was discontinued.

Desocriptine is an ergot alkaloid (alpha-dihydro-beta-ergocryptine) derivative. It is a combined alpha- and beta-adrenoceptor antagonist. Desocriptine is antihypertensive and antianginal agent.

Minaxolone, a water-soluble steroid anesthetic that was studied in 1970s/1980s. It is a positive allosteric modulator of the GABAA receptor. This compound was withdrawn before registration due to reported toxicity in rats.

Metenkephalin (Met-enkephalin) is an endogenous opioid peptide that acts as an agonist at μ-opioid receptors (μORs) and δ-opioid receptors (δORs). Met-enkephalin exhibits neuromodulatory, antinociceptive/analgesic, antidepressant, and gastrointestinal motility modulating activities. Like other endogenous opioids, met-enkephalin modulates expression of opioid receptors and plays a role in reward/reinforcement signaling. Met-enkephalin is also involved in exercise-induced reversal of neuropathic pain and in animals undergoing the forced swim test, decreases immobility time. Met-enkephalin inhibits gastrointestinal muscle contractility, inhibiting motility and gastric emptying. Additionally, analogs of this peptide display anticancer and antiepileptic/anticonvulsant activities.

Conorphone (TR5109) is an opioid of mixed agonist-antagonist analgesic class. In animal models, conorphone demonstrated an analgesic activity in the same range as morphine, and lack of addiction liability. Conoprphone was evaluated in a clinical trial for postoperative pain in the oral surgery model and in patients with postepisiotomy pain. The 40 mg dose of conorphone resulted in a significant incidence of side effects such as drowsiness, dizziness, nausea, and vomiting.

Iliparcil was developed as an orally active beta-D-xyloside venous antithrombotic agent. However, the preclinical studies of this compound were discontinued.

Stenbolone is an anabolic–androgenic steroid of the dihydrotestosterone group patented by Schering AG but never marketed. Ester prodrug of stenbolone is used as an anabolic–androgenic steroid for depot intramuscular injection under the brand names Anatrofin and Stenobolone.

Candocuronium is bisquaternary aza steroid derivative with neuromuscular blocking, ganglion blocking, and vagolytic activities. Its potential adjunctive use in anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation was briefly evaluated in clinical studies in India, but further development discontinued because of attendant cardiovascular effects, primarily tachycardia that was no worse than but also not an improvement over the clinically established pancuronium bromide.

Orconazole, an imidazole derivative, was developed by Janssen Pharmaceutical as an antifungal agent, however, this drug has never been marketed