Ibutamoren (L-163,191 MK-0677) is a spiropiperidine agonist of the ghrelin receptor and a growth hormone secretagogue. Ibutamoren mimics the actions of growth hormone releasing peptide-6 to increase serum levels of serum insulin-like growth factor-I (IGF-I). Orally active Ibutamoren was being developed by Merck & Co. for a variety of indications, including fibromyalgia, muscle wasting/weakness in patients with chronic kidney disease, Alzheimer's disease and fractures.However, there has been no recent development reported or development has been discontinued for these indications.

Arginine vasotocin (Argiprestocin, AVT) is the non-mammalian homologue of arginine vasopressin (AVP) and was first synthesized as an AVP analogue. It was later found in non-mammalian vertebrates and induces similar physiological effects as AVP. AVT is considered the primary antidiuretic hormone. AVT functions to regulate expression of social and reproductive behaviors.

Somatoprim (DG3173) is a heptapeptide somatostatin analog (SSA) that binds with high affinity to sstr2, sstr4 and sstr5 and shows a very low insulin suppression in contrast to other SSA. Initially developed by Ipsen, it is under active development by licensee Aspireo Pharmaceuticals, an Israeli company. In vitro as well as in vivo testing showed a dose-dependent GH lowering effect. Somatoprim has demonstrated a unique receptor binding and pharmacological profile which is differentiated from SSAs that are currently marketed or in clinical development. In particular, Somatoprim has shown an improved side effect profile with reduced adverse effects on the gastrointestinal tract and glucose metabolism. Furthermore, assessment of growth hormone secretion in cultured human somatotroph adenoma tissue treated with Somatoprim indicates that it has the potential to increase the response rate of acromegalic patients to SSA therapy. Somatoprim is currently in phase I/II of clinical development.

Prazarelix is gonadorelin (GnRH) antagonist. It is primarily used in assisted reproduction to control ovulation. The drug works by blocking the action of GnRH upon the pituitary, thus rapidly suppressing the production and action of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Ozarelix is a luteinizing hormone-releasing hormone (LHRH) antagonist. It is known that LHRH antagonist exerts rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones. Thus this inhibitor can be effective in a variety of hormonally dependent disease including prostate cancer, benign prostatic hyperplasia (BPH), and endometriosis. Ozarelix was developed for the treatment of all these diseases including Alzheimer's disease. However, in January 2010 Spectrum Pharmaceuticals announced that it was discontinuing development of ozarelix in BPH. Because the low-dose intermittent therapy was disappointing in the treatment of lower urinary tract symptoms in men with BPH. The development of the drug for Alzheimer's disease was also discontinued. Ozarelix completed phase II trials for the treatment of prostate cancer and is in preclinical trials for the treatment of endometriosis and ovarian cancer.

Depreotide is an ingredient in the diagnostic aid (radioactive imaging agent). Technetium Tc 99m labeled depreotide is a scintigraphic imaging agent that identifies somatostatin receptor-bearing pulmonary masses in patients presenting with pulmonary lesions on computed tomography and/or chest x-ray who have known malignancy or who are highly suspect for malignancy. Adverse events were evaluated in clinical studies of 647 adults. Deaths did not occur during the clinical study period. After Technetium Tc 99m Depreotide Injection, serious adverse events were not reported. Headache was the most commonly reported adverse event. EMA withdrew depreotide containing agent NeoSpect.

Lutrelin is an agonist of gonadotropin-releasing hormone receptor exerting antineoplastic properties.

Selepressin (FE 202158) was designed as a selective and short-acting vasopressin type 1a receptor (V(1a)R) agonist. This drug was developed for the treatment of vasodilatory hypotension in shock. Selepressin successfully completed phase IIa clinical trial, where was found that in septic shock patients, selepressin 2.5 ng/kg/minute was able to rapidly replace norepinephrine, improve fluid balance and shorten the time of mechanical ventilation.

Detirelix is a synthetic decapeptide containing five D-amino acids. It is a very potent Gonadotropin-releasing hormone (GnHR) antagonist. The acute effects of detirelix were consistent with peripheral vasodilation. Subchronic effects were associated with inhibition of pituitary gonadotropic and gonadal hormone secretion. As long-acting GnRH antagonist detirelix can rapidly suppress gonadotropin secretion, inhibit follicular development, and prevent ovulation. It can be used as luteolytic agent. A projected use is for the treatment of sex hormone-releasing diseases, as part of anticancer hormone therapy of sex-hormone-dependent tumors.

Kintor Pharma is developing proxalutamide (developmental code GT-0918), an androgen receptor antagonist, for the treatment of metastatic castrate-resistant prostate cancer and AR-positive triple-negative breast cancer. Proxalutamide is involved in phase III clinical trials in China and in phase II in the USA for patients with metastatic castrate-resistant prostate cancer. In addition, the drug participates in phase I clinical trials for the treatment of AR-positive triple-negative breast cancer. Proxalutamide is expected to become a more effective, less toxic second-generation AR antagonist, which will have a bright prospect once it receives approval for coming on the market.