Mavatrep (JNJ-39439335) is a TRPV1 antagonist. It exerts analgesic potential. Mavatrep demonstrated sustained pharmacodynamic effects (heat pain perception, heat pain latency, capsaicin-induced flare), and an efficacy signal in participants with osteoarthritis

Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor with antihyperlipidemic activity. Microsomal triglyceride transfer protein (MTP) is essential for the synthesis of both chylomicron in the intestine and very low-density lipoprotein in the liver. In an animal model, inhibition of MTP by implitapide reduced both total cholesterol and triglyceride levels and suppressed progression of atherosclerotic lesions in apolipoprotein E knockout mice fed a Western-type diet.

Darodipine is a calcium channel blocking drug, developed by Sandoz in the early 1980s. It potently and selectively antagonizes calcium-induced contraction, decreases the rate of spontaneously beating guinea-pig and rabbit atria. In open-chest dogs, darodipine increased coronary flow and cardiac output, lowered blood pressure, and tended to decrease heart rate while the myocardial contractile force was unchanged. Administration of darodipine led to a significant reduction in mortality and in the severity of neurological symptoms in various types of experimental brain ischemia. Clinical trials demonstrated efficacy for the treatment of stable angina pectoris. In the pilot trial, darodipine was found to be safe but not effective in patients with acute ischemic cerebral infarction.

Menogaril is a semisynthetic derivative of the anthracycline antineoplastic antibiotic nogalamycin. Biochemical studies indicated that, in comparison to doxorubicin, menogaril is bound weakly to DNA, inhibits RNA synthesis less, and has different cell cycle phase-specific cytotoxicity. Menogaril acts as a cleavable complex-stabilizing topoisomerase II inhibitor. Menogaril has been studied in the treatment of various cancers.

Metipirox was developed as a bactericide agent. Information about the current use of this compound is not available

Myfadol is a phenacylpiperidine derivative patented by Tanabe Seiyaku Co., Ltd as low molecular weight non-peptide analgesic. Myfadol produces hot-plate analgesia in rodents with minimal side-effects, and when given parenterally in humans produces analgesia to experimentally-produced and postoperative pain.

Brobactam is a synthetic inhibitor of beta-lactamases produced by both gram-positive and gram-negative bacteria. Brobactam potentiates the antibacterial activity of ampicillin against a wide range of clinically important bacterial strains which produce beta-lactamase. No resistant sub-population was observed amongst the strain s of staphylococci studied, and the development of resistance in vitro was not recorded in individual strains of Staphylococcus aureus and Escherichia coli exposed to subinhibitory concentrations of ampicillin/brobactam. Reduced sensitivity was observed in the case of one strain of M. morganii, which was known to produce an inducible chromosomal cephalosporinase.

Lemuteporfin is a newly introduced, light-sensitive drug for use in combination photodynamic therapy (PDT). It acts on mitochrondria to initiate the apoptotic cascade resulting in cell death (apoptosis). The photosensitizer was highly potent, killing cells at low nanomolar concentrations upon exposure to activating light. The cellular uptake of lemuteporfin was rapid with maximum levels reached within 20 min. Mitogen-activated lymphoid cells accumulated more of the lemuteporfin than their quiescent equivalents, supporting selectivity. Lemuteporfin had been in phase II clinical trials for the treatment of benign prostatic hypertrophy. It is in phase I clinical trials for the treatment of acne rosacea.

Picenadol is a 4-phenylpiperidine derivative and a racemic mixture whose mixed agonist-antagonist properties are a consequence of the d-isomer being a potent opiate agonist, whereas the I-isomer is an opioid antagonist. In the mouse writhing and rat tail heat tests, the analgesic potency of picenadol is estimated to be 1/3 that of morphine. Picenadol itself has weak antagonist activity, whereas the antagonist potency of the l-isomer is approx. 1/10 that of nalorphine. Picenadol has high affinity for both the mu and delta receptors but a markedly lower affinity for the kappa receptor. Extensive pharmacological investigations show picenadol to have a low potential to produce opiate-like side effects, including a low liability for abuse and physical dependence. Antinociceptive properties of picenadol arise from mu agonist actions of the dextrorotatory isomer and that the levorotatory isomer acts to limit the efficacy of the racemate.