Pfizer was developing PF-03814735, an orally administered, reversible inhibitor of the Aurora A and Aurora B kinases. In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1 (Thr 232, a sensitive marker of Aurora1 activity, with IC50 ~ 20 nM), phosphohistone H3 (with IC50 50 nM), and phospho-Aurora2 (with IC50 150 nM). PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. A recent research indicates small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735. PF-03814735 was under Phase I trials for patients with advanced solid tumors, but later this research was discontinued.

Fluorfenidine F-18 is a radionucleotide used in positron emission tomography (PET) imaging procedures.

D-Methyldopa is an inactive isomer of methyldopa. It is known, that only L-isomer has the ability to inhibit dopa decarboxylase and possesses the antihypertensive activity in man. Moreover, about twice the dose of the racemate (DL-form of methyldopa) is required for the equal antihypertensive effect.

Mallinckrodt (previously Sucampo Pharmaceuticals) is developing nobiprostolan (RK 023), a topical therapy for male pattern baldness (androgenetic alopecia) and hypotrichosis. The drug is a physiologically active fatty acid derivative. Nobiprostolan is in Phase IIa clinical trials for the treatment of male pattern baldness.

Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. Dihydrexidine was shown to stimulate cyclic AMP synthesis just as well or better than dopamine. It was the first dopamine D1 receptor agonist that had potent antiparkinsonian activity in a primate model of Parkinson's disease. Dihydrexidine produces hypothermia. Dihydrexidine has been shown to alleviate cognitive deficits or enhance cognitive performance in a number of animal models of cognition. It is under investigation for the improving the cognitive and working memory deficits in schizophrenia and schizotypal disorder.

Linarotene is arotinoid derivative. It is an antikeratolytic agent. Linarotene had been in preclinical phase by Ortho Pharmaceutical (Johnson & Johnson) and BASF Pharma for the treatment of skin disorders. However, this research was discontinued.

AZD-8330 is a potent, selective, orally active MEK inhibitor that blocks signal transduction pathways implicated in cancer cell proliferation and survival. AZD-8330 has shown tumor suppressive activity in multiple preclinical models of human cancer including melanoma, pancreatic, colon, lung, and breast cancers. AZD-8330 specifically inhibits mitogen-activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. AZD-8330 had been in phase I clinical trials by AstraZeneca for the treatment of malignancies. However, this research has been discontinued.

AZD-7687 is a potent inhibitor of Diacylglycerol O-acyltransferase 1 (DGAT1) which was developed by AstraZeneca for the treatment obesity and type 2 diabetes mellitus. AZD-7687 reached phase I of clinical trials, but was discontinued by unknown reasons.