F-901318 (Olorofim) is an orotomide antifungal drug. An investigation into the mechanism of action of F-901318 found that it acts via inhibition of the pyrimidine biosynthesis enzyme dihydroorotate dehydrogenase (DHODH) in a fungal-specific manner. Olorofim is being developed by F2G for the treatment of mycoses.

MK-1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist. Exhibits no binding at the GRP109B receptor. This drug had been in phase II clinical trial for the treatment of atherosclerosis and Dyslipidemia. But then, according to Merck, elevation of HDL cholesterol relative to placebo did not meet the trial's pre-specified primary objective for efficacy; no safety signals were implicated as drivers of the decision to discontinue development.

DSM265 is an experimental antimalarial that selectively inhibits the parasite dihydroorotate dehydrogenase (DHODH). DSM265 is the first DHODH inhibitor to reach clinical development for treatment of malaria. DSM265 is highly selective toward DHODH of the malaria parasite Plasmodium, efficacious against both blood and liver stages of P. falciparum, and active against drug-resistant parasite isolates. The only possible DSM265-related adverse event was a moderate transient elevation in serum bilirubin.

GNF-156 (ganaplacide or KAF-156) is an antimalarial agent that is part of the imidazolopiperazine family. It exerts activity against pre-erythrocytic liver stages, asexual and sexual blood stages. An improvement compared to existing antimalarial drug combinations is that this compound shows promising single-dose antimalarial activity, and no serious safety and tolerability concerns in humans are known so far. Phase II clinical trials have been completed for GNF-156. Its potential is also being investigated in combination with lumefantrine (an aryl-amino alcohol) in LUM-KAF156.

MK 3577 is an orally active glucagon receptor antagonist which was under development by Merck & Co for the treatment of type 2 diabetes mellitus. MK 3577 demonstrate activity in cellular models and preclinical trials. In phase II clinical trials MK 3577 shows good efficacy and acceptable level of adverse events, but no further development reports were published.

Bristol-Myers Squibb developed BMS-929075 as a selective, orally bioavailable hepatitis C virus (HCV) NS5B polymerase inhibitor for the treatment of chronic HCV infection. BMS-929075 was involved in phase I clinical trials for hepatitis C virus (HCV) infected patients; however, the company withdrew a study prior to enrolment.