Milataxel, a taxane that binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization. Milataxel has completed phase II clinical trials for non-small cell lung cancer patients, and for colorectal cancer patients. Besides, it was studied for malignant mesothelioma. However, the drug has been discontinued due to toxicity issues at the dose level of 35 mg/m 2.

PF-06747775 is an irreversible pyrrolopyrimidine inhibitor of epidermal growth factor receptor (EGFR) T790M mutants which provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties. The third-generation class of EGFR tyrosine kinase inhibitors PF-06747775 is a clinical candidate drug for treatment of non-small-cell lung cancer (NSCLC) driven by mutant EGFR.

GW-493838 was developed by GlaxoSmithKline as an adenosine A1A receptor agonist for the treatment of dyslipidemia and neuropathic pain. GW493838 participated in the phase II clinical trial to determine the analgesic effect in patients with post-herpetic neuralgia or peripheral nerve injury caused by trauma or surgery. However, this study has been discontinued.

Cipargamin is an experimental synthetic antimalarial molecule belonging to the spiroindolone class. It possesses both the potency (average IC50 of 550 pM against asexual blood-stage P. falciparum) and favorable pharmacokinetics (elimination half-life of ~24 hours in humans) needed for a single-dose cure, a feature that could help slow the onset of parasite resistance and that is not shared by existing, approved antimalarial drugs. KAE609 is also unique in its ability to block transmission to mosquitoes. Cipargamin is a parasite P-type ATPase4 inhibitor. Cipargamin in phase II clinical trials for the treatment of acute, uncomplicated malaria due to plasmodium falciparum monoinfection. Nausea was the most common reported adverse effect. The adverse events were generally mild and did not lead to any discontinuations of the drug.

Elacridar is an oral bioenhancer that targets multiple drug resistance in tumors. Elacridar is a strong and relatively specific inhibitor of P-gp and BCRP, two main efflux transporters. Development of elacridar is assumed to have been discontinued.