CP-866087 is a mu opioid receptor antagonist, discovered by Pfizer. The compound was able to antagonize the effect of morphine in a rodent tail flick assay and produced a dose-dependent decrease in alcohol intake in alcohol-preferring rats. The compound was investigated in clinical trials for the treatment of obesity, alcoholism and female sexual arousal disorder. In the later study, although improvements were seen with CP-866,087 in the key efficacy endpoints, there was no clinical treatment benefit over placebo.

PF-00610355 is ultra long-acting beta 2 adrenergic receptor-agonists that is being developed for ‘once daily’ treatment of asthma. Plasma pharmacokinetics of orally inhaled PF-00610355 are consistent and exhibit a sustained plateau after single/multiple doses, but plasma exposure is reduced in asthmatic patients compared with healthy volunteers. Although substantial increases in heart rate were observed in healthy volunteers, both pharmacokinetic as well as pharmacodynamic differences between healthy volunteers and chronic obstructive pulmonary disease (COPD) patients (the systemic exposure of PF-00610355 is substantially lower in COPD than in healthy volunteers) explain the modest effect of PF-00610355 on heart rate in the patient population. PF-00610355 had been in phase II clinical trials for the treatment of asthma and chronic obstructive pulmonary disease. However, this development was discontinued.

Pocapavir is a capsid-binding molecule. It is a capsid inhibitor that blocks virus uncoating and viral RNA release into cells, which in turn prevents virus replication. Pocapavir is a potent, selective, anti-enterovirus molecule with in vitro and in vivo activities. Antiviral testing against viruses of the 15 most commonly isolated enterovirus serotypes indicates that pocapavir inhibits 80% of the immunotypes (154 viruses) at a concentration that is within the levels of the molecule achievable in plasma after oral dosing in higher animals. Persistent low viral load after therapy completion may indicate lack of antiviral effect from pocapavir for neonatal enteroviral sepsis treatment. Pocapavir had been in phase II clinical trial for the treatment of poliomyelitis but no recent reports on development were identified.

PF-05175157 exhibited good potencies against the two isoforms of the Acetyl-CoA carboxylase enzyme (ACC1 and ACC2) from human and rat. PF-05175157 has undergone multiple clinical trials in healthy volunteers and for the treatment of diabetes mellitus. PF-05175157 was in the phase II when the development was discontinued due to safety concerns. Among potential barriers for the use of ACC inhibitors in humans include concerns of increased risk of myocardial injury following an ischemic event. PF-05175157 reduced the multiplication of West Nile virus (WNV), dengue virus (DENV), and Zika virus (ZIKV) in cultured cells, which is compatible with the predicted broad spectrum of host targeting antivirals. PF-05175157 reduced the peak of viremia in WNV-infected mice, supporting that ACC is a valuable target for antiviral intervention. PF05175157 also reduced the viral burden in the kidney of infected mice.

Sapitinib is an oral, reversible and equipotent inhibitor of EGFR, HER2 and HER3 signalling. The drug was tested in phase II of clinical trials in patients with breast cancer, colorectal cancer, gastric cancer and NSCL carcinoma, however its development for breast cancer therapy seems to be terminated. Sapitinib absorption is rapid and the drug is totally cleared by metabolism with the major routes being oxidation and amine or ether cleavage around the piperidine ring with subsequent glucuronide or sulphate conjugation.