CPG-52852 (PF-04878691) is a toll-like receptor 7 (TRL7) agonist. The drug was developed by 3M Pharmaceuticals and the Coley Pharmaceutical Group and was investigated in a number of clinical trials in patients with advanced cancer. Sustained tolerability and modest clinical benefit were demonstrated in heavily pretreated recurrent breast, ovarian, and cervix cancers. After Coley was acquired by Pfizer in 2007, the drug was repurposed for the treatment of hepatitis C. A phase 1 clinical trial was conducted. The development of the compound was discontinued because the compound was believed to unlikely to achieve the proof-of-concept criteria as a result of pharmacodynamic modeling.

Murabutide is a safe synthetic immunomodulator derived from muramyl dipeptide, the smallest bioactive unit of bacterial peptidoglycan. In contrast to muramyl dipeptide, Murabutide is devoid of pyrogenic activity and lacks somnogenic activity. Murabutide acts as a ligand for the intracellular receptor NOD2 and has the capacity to synergize with selected therapeutic cytokines to drive the release of Th1 cytokines. Murabutide has been found to suppress human immunodeficiency virus type-1 (HIV-1) replication, in macrophages, through regulated expression of cellular factors needed at different steps in the virus replication cycle.

Elbanizine [HWA 214] is an antihistamine which was undergoing preclinical trials with Hoechst Marion Roussel in Germany for the treatment of allergic asthma. Elbanizine does not have such drawbacks as causing drowsiness or being effective only as a prophylactic drug, and could provide advantages over other non-sedative compounds, such as terfenadine and astemizole, in that it is water soluble and thus can be administered through inhalation or through intravenous application.

Etomoxir is an irreversible inhibitor of carnitine O-palmitoyltransferase (CPT) I. It inhibits fatty acid oxidation and fatty acid and cholesterol synthesis in an enantiomer-selective manner: only the R-enantiomer of etomoxir inhibits fatty acid oxidation, S-enantiomer inhibits fatty acid and cholesterol synthesis but not fatty acid oxidation. Etomoxir was studied for the treatment of congestive heart failure and type II diabetes, however, its development was discontinued.

Pinafide is a rodenticide and anti-protozoal agent. Pinafide shows strong cytostatic activity against both HeLa and KB cells and is moderately toxic to both mice and rats. It has been proved active against experimental tumors and shown to be inhibitor of two DNA viruses. Pinafide blocks cell growth by inhibiting DNA and RNA synthesis. It has been shown to bind to double-helical DNA by intercalation. Pinafide inhibited the activity of M. tuberculosis NAD⁺-dependent DNA ligase A at concentrations of 50 uM. At the chemical screening was found that pinafide inhibited B-Myb transcriptional activity in luciferase assays. The cross placental-barrier studies showed that 3H-pinafide was present in the 14-day fetuses.

Ersentilide (CK-3579 or HE93) is a blocker of beta1-adrenergic receptors and potassium channels. It exerts class III antiarrhythmic activity. It prevents ventricular fibrillation in a canine model of lethal arrhythmias.

Erbulozole (R 55104) is a water soluble congener of the microtubule inhibitor tubulozole, which has proven to possess anti-invasive, antitumoral and radiosensitizing capacities. Erbulozole development for the treatment of cancer has been discontinued.

Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.

Agouron (Pfizer) was developing AG-24322 (AG-024322), a small-molecule cyclin-dependent kinase (CDK) inhibitor, for the treatment of cancer. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. AG-24322 is a potent ATP-competitive inhibitor of CDK1, CDK2, and CDK4 with Ki values in the 2–3 nM range and selectivity over other non-CDKs. This compound has been shown to inhibit Rb phosphorylation in cells, elicit cell-cycle arrest, and have antiproliferative activity in multiple human tumor cell lines (IC50 values from 30 to 200 nM). AG-24322 was reported to be undergoing phase I trials for cancer in the US, however the development was discontinued.

Sopromidine is a neuroprotective drug. Sopromidine is a potent and stereoselective isomer of the achiral H2-agonist impromidine. The chiral impromidine isomer sopromidine is of special interest as the (R)-configurated compound behaves as gpH2R agonist, whereas the (S)-configurated counterpart is devoid of agonist activity. Both Sopromidine and its S enantiomer acted as antagonists of histamine at H3-autoreceptors with similar potencies (Ki = 5.6 X 10(-8) M and 4.5 X 10(-8) M), whereas Sopromidine acted as an H2-receptor agonist and the S-enantiomer as an H2-receptor antagonist.