Ciraparantag (PER-977, aripazine), developed by Perosphere Inc., is a small, synthetic, water-soluble, cationic molecule and can reverse the anticoagulation mediated by unfractionated heparin, low-molecular-weight heparin, factor Xa and factor IIa inhibitors, and fondaparinux. It has the potential to be a universal antidote, inhibiting nearly all anticoagulants except vitamin K antagonists and argatroban. In April 2015, ciraparantag received FDA fast-track designation as an investigational anticoagulant reversal agent. Phase I/II trials are currently underway to evaluate the safety and efficacy of PER977 in reversing anticoagulation of edoxaban, LMWH, and UFH.2.

Seglitide (previously known as L363,586 or MK-678), a cyclic, hexapeptide analog of somatostatin-14, is a somatostatin receptor 2 (SSTR2) agonist. This compound was studied in Alzheimer's disease. Besides, it possessed inhibitory actions on rat growth hormone (GH) release and thus could have a role in the treatment of acromegaly. Intravenous and intranasal administration of seglitide to diabetic subjects was effective in reducing both fasting and postprandial hyperglycemia. Thus, this compound could be useful in the control of unstable diabetes. In addition, preclinical studies have shown that seglitide had potential as a treatment for diabetic retinopathy and macular degeneration. However, the further studied of this compound were discontinued.

Cormethasone is a topical antiinflammatory corticosteroid discovered by Du Pont.

Acetorphine is a synthetic narcotic analgesic. Acetorphine was reported to have uses in veterinary medicine with pronounced advantages in the immobilization of the giraffe in which toxic effects were reduced as compared to the effects of etorphine. In July 1966, the Director-General of the World Health Organization informed the Secretary-General that WHO had arrived at the conclusion that etorphine and acetorphine should be included in Schedule I of the Convention, since they could give rise to similar abuse, and produce similar ill effects as the substances already listed therein. Acetorphine is a Schedule I controlled substance in the United States.

Telapristone is an orally available 21-substituted-19-nor-progestin and selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Its acetate form, the telapristone Acetate is a clinically used and a studied drug.

FERTIRELIN is an analog of luteinizing hormone releasing factor. The drug has been used since 1981 in Japan to treat various types of reproductive failure in cattle.

Dirucotide (MBP 8298) is a synthetic myelin basic protein (MBP) peptide designed to decrease type 2 helper T cells (TH2)-mediated B-cell signalling of auto-reactive T-cells thereby reducing the production of specific antibodies that target endogenous MBP. MBP is the dominant site of attack in patients with multiple sclerosis and haplotype (HLA) DR2 or DR4. Dirucotide did not meet the primary endpoint of delaying disease progression, as measured by the Expanded Disability Status Scale (EDSS), during the two-year MAESTRO-01 Phase III trial in patients with secondary progressive multiple sclerosis (SPMS). In addition, there were no statistically significant differences between dirucotide and placebo on the secondary endpoints of the study. After disappointing trial results, development of the drug was ended in 2009.

Clomegestone (clomagestone) is an investigational steroidal progestogen. Clomegestone exhibits anti-estrogenic activity in estrone stimulated immature mice when administered orally at 100 ug.

Sotrastaurin, an orally-active, first-in-class immunomodulator, is under development by Novartis for the treatment of uveal melanoma and diffuse-large B-cell lymphoma. Sotrastaurin is a low molecular mass synthetic compound that potently inhibits the PKC α, β and the θ isoforms resulting in selective NF-κB inactivation. Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay. Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine protein kinases overexpressed in certain types of cancer cells, is involved in cell differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes. Sotrastaurin is currently in phase II trials by Novartis for the treatment of large B-cell lymphoma and uveal melanoma. Sotrastaurin was in Phase II of clinical development for the prevention of acute rejection after solid organ transplantation and psoriasis, but this reseach had being discontinued.