Fasidotril is a diester prodrug of the active metabolite fasidotrilat. Fasidotrilat inhibited both angiotensin I converting enzyme (ACE, EC 3.4.25.1) and neprilysin (NEP, EC 3.4.24.11, also named neutral endopeptidase, enkephalinase, or atriopeptidase) at nanomolar concentrations (Ki = 9.8 nM against ACE and 5.1 nM against NEP) Fasidotril was being developed for the treatment of myocardial infarction, congestive heart failure and myocardial infarction.

Mannomustine is a substance synthesized as one of a series of compounds linking the actively cytotoxic chemical group beta-chlorethylamine with a naturally occurring substance, mannitol. Mannomustine is an alkylating agent with antineoplastic properties. It was being studied in the treatment of hematologic malignancies.

Leucinocaine is the local anaesthetic with actions similar to lignocaine. It has been used by topical application for local pain relief.

AFN-1252 (now known as Debio-1452) is an antibiotic drug which is in phase II of clinical trials for the treatment of Staphylococcal skin and skin structure infections. The drug was effective in vitro against all isolates of S.aureus and its effect was explained by inhibition of enoyl-acyl carrier protein Reductase (FabI).

COTI-2 is an orally available small molecule targeting p53, a tumor suppressor gene that is mutated in over 50% of all cancers. The drug was developed by Clinical Outcome Technologies Inc (now Cotinga Pharmaceuticals) and is believed to act by reactivating mutant p53 and inhibiting the phosphatidylinositol 3-kinase (PI3K)/Akt. The drug is being evaluated in phase I clinical trials for the treatment of gynecologic cancers and head and neck squamous cell carcinoma.

Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.

Dimethylthiambutene is the synthetic narcotic analgesic agent. It has analgesic effect similar to those of meperidine. The (+)-enantiomer of dimethylthiambutene is more active than the (-)-isomer. Dimethylthiambutene clinically compared with meperidine (pethidine), but maintains the dependence-producing capability of morphine. It has had illicit use in Japan in the past. Dimethylthiambutene is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.

Pentacynium bis-methylsulphate (presidal) is a salt of pentacynium, which was studied as a ganglion-blocking agent to treat hypertension. Glaxo Wellcome developed this drug; however, information about the further use of pentacynium is not available.

CPI-0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor CPI-0610 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. CPI-0610 is currently being evaluated in three Phase 1 clinical trials in the U.S.

Biclofibrate was investigated as an antilipidemic agent.