Delcasertib is a peptide inhibitor of protein kinase C-delta, developed by KAI Pharmaceuticals. Delcasertib disrupts binding of delta-PKC to its receptor for activated C kinase, thereby preventing localization of delta-PKC to the mitochondria during periods of myocardial ischemia and reperfusion. In preclinical studies, when given as a single intracoronary dose, delcasertib reduced infarct size, enhanced early recovery of regional left ventricular contractility, and improved microvascular patency and function in animal models of acute myocardial infarction. The compound diminished myocardial necrosis and improved reperfusion in a pilot study during the primary percutaneous coronary intervention (PCI) for ST-elevation myocardial infarction (STEMI). In a larger clinical trial, however, intravenous infusion of delcasertib during PCI for acute STEMI in a population of patients treated according to the contemporary standard of care did not reduce biomarkers of myocardial injury.

Forigerimod (also known as IPP-201101) a phosphopeptide is being investigated for the treatment of Lupus Erythematosus, Systemic. This drug is completed phase III clinical trials and is ready for licensing.

Anaritide (Auriculin-Registered Trademark) is a 25-amino-acid synthetic form of atrial natriuretic peptide. Scios Nova was developing anaritide acetate for use in the treatment, prevention and diagnosis of acute renal failure, heart failure and hypertension. Scios suspended development of AURICULIN® anaritide based upon the results of an interim analysis of data from a 250-patient Phase III study in oliguric acute renal failure. The study was suspended due to the low probability that a positive outcome could be obtained with respect to its primary clinical endpoint, dialysis-free survival.

N-(2-Bromophenyl)-9-Methyl-9-Azabicyclo[3.3.1]Nonan-3-Amine (also known as AT-1001) is a high-affinity and highly selective ligand at α3β4 nicotinic cholinergic receptors (nAChRs) that was reported to decrease nicotine self-administration in rats. AT-1001 has a single-digit nanomolar binding affinity for the α3β4 nAChR and over 100-fold selectivity over the α4β2 nAChR and α7 nAChR in competition binding experiments. In electrophysiological experiments, AT-1001 had partial agonist activity at the α3β4 nAChR, evoking 35% of maximum ACh response, and at the same doses, produced desensitization of the ACh response, effectively acting as a functional antagonist at the α3β4 nAChR. Interestingly, AT-1001 also selectively decreased self-administration of cigarette smoke extract (CSE), an aqueous extract of cigarette smoke components, without altering natural food intake, when administered systemically to rats trained to self-administer CSE

Lenomorelin (Ghrelin) is a pleiotropic hormone, whose effect on growth hormone secretion, through the growth hormone secretagogue (GHS) receptor, is one of its many actions. It is synthesized principally in the stomach. Ghrelin-producing cells constitute a distinct group of endocrine cells dispersed throughout the gastric mucosa and to a lesser extent in the small intestine and the endocrine pancreas. Ghrelin plasma levels rise during fasting and chronic caloric restriction to stimulate food intake and fat storage and to prevent life-threatening falls in blood glucose. Plasma ghrelin levels decrease after a meal is consumed and in conditions of energy surplus (such as obesity). Ghrelin has emerged as a key player in the regulation of appetite and energy homeostasis. It stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. Ghrelin levels are negatively correlated with body mass index (BMI) and insulin resistance. Lenomorelin is a peptide of 28 amino acids, in which the serine 3 residue is n-octanoylated, which is necessary for biological activity.

Rusalatide acetate (also known as chrysalin or TP 508) is a 23-amino acid peptide derived from human prothrombin; it represents part of the receptor-binding domain of the human thrombin molecule. Rusalatide acetate binds to high-affinity thrombin receptors and mimics cellular effects of thrombin at sites of tissue injury. Rusalatide acetate demonstrated safety and potential efficacy in phase I/II clinical trials for the treatment of diabetic foot ulcers. It interacts with cell surface receptors to stimulate a cascade of cellular and molecular wound healing events, including activation of nitric oxide signaling. In addition, this drug participated in phase II clinical trial to determine the effectiveness of four doses for treating broken wrists in adults. However, this study was terminated because the drug did not demonstrate benefit compared to placebo. Rusalatide acetate was also studied as a cardiovascular drug. However, in January 2012, Capstone discontinued the development of rusalatide, for financial reasons. Recent studies show that a single injection of TP508 (rusalatide acetate) administered 24 h after irradiation significantly increases survival and delays mortality in murine models of acute radiation mortality. Thus, this drug is being developed as a potential nuclear countermeasure.