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 Anamorelin

Description of Anamorelin: Anamorelin hydrochloride is the orally bioavailable hydrochloride salt of a synthetic, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). 

Current developer:  Ono Pharmaceutical Co., Ltd. (Osaka, Japan); Rejuvenon Corporation; Sapphire Therapeutics, Inc.; Helsinn Group. 

Anamorelin is currently under development for the management of non-small lung cancer associated cachexia/anorexia.. Ghrelin is a circulating peptide hormone, principally produced in stomach cells, which has various physiological actions, including appetite stimulation and muscle-building (anabolic) effects. Anamorelin has similar physiological actions to those of ghrelin, but, unlike ghrelin itself, is orally active, and therefore could be an innovative treatment to improve impaired quality of life in cancer anorexia/cachexia patients.

Cachexia affects many patients with chronic diseases, including AIDS, cancer, organ failure, and rheumatoid arthritis. Sometimes called "wasting," symptoms include loss of appetite (anorexia) and lean body mass. Cachexia frequently accompanies malignant cancers and is an independent risk factor for poor survival. To date, there are no approved treatments of ghrelin or ghrelin mimetics in the United States, Japan, Korea or Taiwan for cancer anorexia/cachexia. Anamorelin has been granted Fast Track status by the FDA.  (source: http://www.ergogenics.org/rc1291.html).

Current development stage: Phase II and Phase III. (see:http://www.helsinn.com/Institutional.aspx?Root=211&L2=229&L3=230&Lingua=EN).

Highlight of recent research using Anamorelin (RC-1291)

Data published in June 2009.

Pharmacodynamic hormonal effects of anamorelin. OBJECTIVE: Activation of ghrelin receptors stimulates GH secretion and appetite, increasing lean body mass and body weight. However, clinical use of ghrelin is limited because it has a short half-life and must be administered parenterally. Anamorelin is a novel, orally active, non-peptidic ghrelin mimetic and growth hormone secretagogue. Our objective was to evaluate its hormonal effects in healthy subjects. RESULTS: Anamorelin significantly increased GH levels at all doses (p<or=0.01). Effects on the somatotropic axis were maintained, as evidenced by sustained increases in IGF-1 and IGFBP-3 compared to placebo following 5-6 days of treatment. Negligible effects on other anterior pituitary hormone profiles and on fasting glucose were noted and all mean hormone levels remained within normal range. Some degree of insulin resistance as assessed by HOMA-IR was evident after treatment with 75 mg dose but not with the 25 or the 50 mg doses. Significant dose-related increases in body weight were recorded. Changes in body weight directly correlated with changes in IGF-1 levels. Anamorelin was well tolerated. CONCLUSIONS: Anamorelin increases GH, IGF-1, IGFBP-3 and body weight with good tolerability and selectivity, without affecting other anterior pituitary axes or fasting glucose levels. [source: Growth Horm IGF Res. 2009 Jun;19(3):267-73. Epub 2009 Feb 3. Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers. Garcia JM, Polvino WJ. Division of Diabetes, Endocrinology and Metabolism, Michael E. DeBakey Veterans Affairs Medical Center, Baylor College of Medicine, Houston, TX 77030, USA. jgarcia1@bcm.tmc.edu].

Data published in May 2007

Results of phase I safety study using anamorelin: PURPOSE: RC-1291 is a novel, oral ghrelin mimetic and growth hormone (GH) secretagogue being developed to increase appetite and lean muscle mass in patients with cancer-associated anorexia/cachexia. This randomized, double-blind, placebo-controlled, multiple-dose, dose-escalation phase I study in healthy volunteers evaluated RC-1291 once daily (qd) and twice daily (bid) for effect on body weight and safety. RESULTS: Subjects who received RC-1291, 50 or 75 mg, had significant dose-related weight gain after 6 days versus placebo, with the greatest increases seen with daily dosing. The mean increase in weight from baseline after 50 mg qd was 1.25 +/- 0.725 kg (p = .0022 versus placebo), and after 75 mg qd it was 1.16 +/- 0.651 kg (p = .0022 versus placebo). One subject in the 50 mg qd group had moderate transient elevation in aspartate aminotransferase and alanine aminotransferase levels. No other laboratory or clinical adverse events of consequence were reported. CONCLUSIONS: Results indicate that RC-1291 produces dose-related increases in body weight with no dose-limiting adverse effects, and may be an effective treatment for anorexia/cachexia. [source: Oncologist. 2007 May;12(5):594-600. Effect on body weight and safety of RC-1291, a novel, orally available ghrelin mimetic and growth hormone secretagogue: results of a phase I, randomized, placebo-controlled, multiple-dose study in healthy volunteers. Garcia JM, Polvino WJ. Michael E. DeBakey Veterans Affairs Medical Center, Baylor College of Medicine, Houston, Texas 77030, USA. Jgarcia1@bcm.tmc.edu].

1: Morozumi N, Hanada T, Habara H, Yamaki A, Furuya M, Nakatsuka T, Inomata N,Minamitake Y, Ohsuye K, Kangawa K. The role of C-terminal part of ghrelin in pharmacokinetic profile and biological activity in rats. Peptides. 2011 May;32(5):1001-7. Epub 2011 Feb 1. PubMed PMID: 21291937.

2: Garcia JM, Polvino WJ. Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers.Growth Horm IGF Res. 2009 Jun;19(3):267-73. Epub 2009 Feb 3. PubMed PMID:
19196529.

3: Garcia JM, Polvino WJ. Effect on body weight and safety of RC-1291, a novel,orally available ghrelin mimetic and growth hormone secretagogue: results of a phase I, randomized, placebo-controlled, multiple-dose study in healthy volunteers. Oncologist. 2007 May;12(5):594-600. PubMed PMID: 17522248.