An orally bioavailable imidazopyridazine and inhibitor of Janus kinase 2 mutant V617F (JAK2V617F), with potential antineoplastic activity. Upon oral administration, gandotinib selectively and competitively inhibits the activation of JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and the induction of apoptosis in JAK2V617F-expressing tumor cells. Gandotinib is in phase II clinical trials by Lilly for the treatment of myeloproliferative disorders.

Coumermycin is from the aminocoumarin class of antibiotic compounds which acts by inhibiting DNA gyrase. Coumermycin is effective against gram-positive bacteria, but not gram-negative bacteria. Coumermycin its derivatives have been studied since the 1950's as potential antibiotic. However, it has seen little to no clinical development because of its low water solubility, toxicity profile, and ineffectiveness against gram-negative bacteria.

Valspodar (PSC-833) is a derivative of cyclosporin but devoid of the immunosuppressive and nephrotoxic properties seen in cyclosporin A. It exhibited high-affinity binding to Mdr1 P-glycoprotein (P-gp) and demonstrated multidrug resistance-reversing activity superior to cyclosporin A and verapamil both in vitro and in vivo. Preclinical and phase I/II clinical data have indicated that plasma levels of PSC-833 with multidrug resistance-reversing activities are achievable. Potent inhibition of intestinal, hepatobiliary and blood-brain barrier P-gp function has been demonstrated. The toxicity profiles of valspodar are acceptable and dose-limited by transient and reversible cerebellar ataxia. It has shown multidrug resistance-modulating activities towards acute myeloid leukemia, multiple myeloma and ovarian cancer in phase I/II clinical trials. However, the company discontinued development of valspodar in April 2001 following disappointing results reported from several multicentre phase III studies.

Darapladib (SB-435495), as reversible inhibitors of lipoprotein-associated phospholipase A(2) (Lp-PLA(2) has been developed and studies for the potential treatment of atherosclerosis. In November 2013, GSK announced that the drug had failed to meet Phase III endpoints in a trial of 16,000 patients with acute coronary syndrome.

Indatraline (Lu 19-005) is a non-selective monoamine transporter inhibitor that has been shown to block the reuptake of dopamine, norepinephrine, and serotonin with effects similar to those of cocaine. In vivo, indatraline produced behavioral effects suggestive of enhanced dopaminergic, noradrenergic, and serotonergic activity in mice. Indatraline also substituted for a high dose of cocaine in rats trained to discriminate between a low and a high dose of cocaine, which demonstrates that indatraline produces cocaine-like discriminative stimulus effects. Indatraline has been studied to block the action of methamphetamine and MDMA.

Alazanine triclofenate is a mixture of one molecule of 3-ethyl-2-(3-(3-ethyl-2-benzothiazolinylidene)propenyl)benzothiazolium 2,4,5-trichlorophenate and two molecules of 2,4,5-trichlorophenol. It is an antiparasitic agent. It is antimalarial drug, highly active against multiple Plasmodium falciparum isolates with IC50 value of 2.36E-07 M.

Luteolin, 3',4',5,7-tetrahydroxyflavone, is a common flavonoid that exists in many types of plants including fruits, vegetables, and medicinal herbs. Plants rich in luteolin have been used in Chinese traditional medicine for treating various diseases such as hypertension, inflammatory disorders, and cancer. Luteolin possesses a variety of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial and anticancer activities. Numerous studies have shown that luteolin possesses beneficial neuroprotective effects both in vitro and in vivo.

Ranirestat (AS-3201, SX-3030, SX-3202) is an oral aldose reductase inhibitor. (-)-enantiomer (AS-3201) is 10 times more potent in inhibition of the aldose reductase and 500 times more potent in the in vivo activity than the corresponding (+)-enantiomer (SX-3202). Ranirestat is being developed by Dainippon Sumitomo Pharma (formerly Dainippon Pharmaceutical) for the treatment of diabetic complications, primarily diabetic neuropathy. Ranirestat is a well-tolerated front-line inhibitor. It reproducibly exhibits some degree of measurable objective beneficial outcomes in diabetic neuropathy.