Anamorelin

Anamorelin
Systematic (IUPAC) name
2-Amino-N-[(2R)-1-[(3R)-3-benzyl-3-[dimethylamino(methyl)carbamoyl]piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide
Clinical data
Routes of
administration		 Oral
Pharmacokinetic data
Biological half-life 6–7 hours[1]
Identifiers
CAS Number 249921-19-5
ATC code None
PubChem CID 9828911
ChemSpider 8004650
Chemical data
Formula C31H42N6O3
Molar mass 546.70358 g/mol

Anamorelin (INN) (developmental code names ONO-7643, RC-1291, ST-1291), also known as anamorelin hydrochloride (USAN, JAN), is a non-peptide, orally-active, centrally-penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) with appetite-enhancing and anabolic effects which is under development by Helsinn Therapeutics for the treatment of cancer cachexia and anorexia.[2][3][4]

Anamorelin significantly increases plasma levels of growth hormone (GH), insulin-like growth factor 1 (IGF-1), and insulin-like growth factor-binding protein 3 (IGFBP-3) in humans, without affecting plasma levels of prolactin, cortisol, insulin, glucose, adrenocorticotropic hormone (ACTH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or thyroid-stimulating hormone (TSH).[3][5] In addition, anamorelin significantly increases appetite, overall body weight, lean body mass, and muscle strength,[4][5] with increases in body weight correlating directly with increases in plasma IGF-1 levels.[3]

As of June 2015, anamorelin is in several phase III clinical trials for the treatment of cancer cachexia and anorexia associated with non-small-cell lung carcinoma.[6]

See also

References

  1. ↑ Leese, Philip T.; Trang, John M.; Blum, Robert A.; de Groot, Eleanor (2015). "An open-label clinical trial of the effects of age and gender on the pharmacodynamics, pharmacokinetics and safety of the ghrelin receptor agonist anamorelin". Clinical Pharmacology in Drug Development 4 (2): 112–120. doi:10.1002/cpdd.175. ISSN 2160-763X.
  2. ↑ Currow, David C; Abernethy, Amy P (2014). "Anamorelin hydrochloride in the treatment of cancer anorexia-cachexia syndrome". Future Oncology 10 (5): 789–802. doi:10.2217/fon.14.14. ISSN 1479-6694.
  3. 1 2 3 Garcia, José M.; Polvino, William J. (2009). "Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers". Growth Hormone & IGF Research 19 (3): 267–273. doi:10.1016/j.ghir.2008.12.003. ISSN 1096-6374.
  4. 1 2 Garcia, José M; Boccia, Ralph V; Graham, Charles D; Yan, Ying; Duus, Elizabeth Manning; Allen, Suzan; Friend, John (2015). "Anamorelin for patients with cancer cachexia: an integrated analysis of two phase 2, randomised, placebo-controlled, double-blind trials". The Lancet Oncology 16 (1): 108–116. doi:10.1016/S1470-2045(14)71154-4. ISSN 1470-2045.
  5. 1 2 Garcia, José M.; Friend, John; Allen, Suzan (2012). "Therapeutic potential of anamorelin, a novel, oral ghrelin mimetic, in patients with cancer-related cachexia: a multicenter, randomized, double-blind, crossover, pilot study". Supportive Care in Cancer 21 (1): 129–137. doi:10.1007/s00520-012-1500-1. ISSN 0941-4355.
  6. ↑ Zhang, Hongjie; Garcia, Jose M (2015). "Anamorelin hydrochloride for the treatment of cancer-anorexia-cachexia in NSCLC". Expert Opinion on Pharmacotherapy 16 (8): 1245–1253. doi:10.1517/14656566.2015.1041500. ISSN 1465-6566.

External links


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