Alvocidib (also known as Flavopiridol or HMR-1275) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia, by Tolero Pharmaceuticals, Inc. As a broad spectrum CDK inhibitor, Alvocidib can inhibit cell cycle progression in either G1 or G2 and induces G1 arrest in either MCF-7 or MDA-MB-468 cells by inhibition of the CDK4 or CDK2 kinase activity. Alvocidib exhibits potent cytotoxicity against a wide variety of tumor cell lines (LNCAP, HCT116, A2780, K562, PC3, and Mia PaCa-2) with IC50 values ranging from 16 nM for LNCAP to 130 nM for K562. Administration of Alvocidib at 7.5 mg/kg for 7 days displays slight antitumor activity against P388 murine leukemia, and active against the human A2780 ovarian carcinoma implanted sc in nude mice). Alvocidib treatment at 1-2.5 mg/kg for 10 days significantly suppresses collagen-induced arthritis in mice in a dose-dependent manner, by inhibiting synovial hyperplasia and joint destruction, whereas serum concentrations of anti-collagen type II (CII) Abs and proliferative responses to CII are maintained. Tolero Pharmaceuticals Inc. announced that the FDA has granted orphan drug designation for Alvocidib, its cyclin-dependent kinase small molecule inhibitor, for the treatment of patients with acute myeloid leukemia.

Nonaperone, a butyrophenone, is a neuroleptic agent. It is antipsychotic in schizophrenics at doses which do not elicit extrapyridal side effects.

Praxadine is the anti-inflammatory and analgesic agent. Praxadine inhibited the activity of purified inducible NOS (iNOS), endothelial NOS (eNOS), and neuronal NOS (nNOS) isoforms to a similar extent.

Omaciclovir (previously known as H2G), a cyclic guanosine analog that is structurally similar to acyclovir and was in clinical development for the treatment of herpesvirus infections. This drug acted against varicella-zoster virus (VZV), by the formation of high concentrations of relatively stable H2G-triphosphate, which is a potent inhibitor of the viral DNA polymerases. However, further development of this drug was discontinued.

Minalrestat was developed by Wyeth-Ayerst as an aldose reductase inhibitor. It is known, the aldose reductase inhibition might ameliorate diabetic complications through the correction of the altered microvascular reactivity by a mechanism that involves NO and membrane hyperpolarization. That is why minalrestat was studied for patients with diabetic retinopathy. However, Wyeth discontinued development of minalrestat.

Tinabinol is a thiopyranobenzopyran derivative patented by Sharps Associates as tranquilizing agent. In preclinical modes Tinabinol shows good analgesic properties and causes ataxia in dogs at low doses.

Lombazole is an antimicrobial agent of the imidazole class. It induced profound ultrastructural changes in Staphylococcus epidermidis and Candida albicans. Like other members of the imidazole series, such as clotrimazole, miconazole, and bifonazole, the compound has a broad spectrum of activity. It is active against several budding and filamentous fungi as well as gram-positive bacteria. Lombazole most probably interferes with fungal lipid synthesis by inhibiting sterol C-14 demethylation. Lipid biosynthesis is the primary site of action of lombazole in the bacterium Staphylococcus epidermidis. Lombazole was recommended against akne.

Nictindole is a non-steroidal anti-inflammatory agent. It is a thromboxane synthetase inhibitor. Nictindole inhibits generation of TXA2 in human platelet rich plasma.

Dabelotine is a cognitive-enhancing drug, developed by Servier. The drug has been shown to improve some aspects of cognitive processes, such as attention, curiosity, motivation, acquisition, and recall of memory. Dabelotine has also been shown to reduce the effect of an anticholinergic drug such as scopolamine. The drug increases the in vitro K+-induced norepinephrine release in rodent cerebral slices, and have no effect on noradrenergic and cholinergic receptor binding sites. Dabelotine was investigated in phase 2 clinical trials for the treatment of dementia, where it was demonstrated that 50-mg and 100-mg doses produced an improvement in reaction time and performance in memory tasks.