Anamorelin
Orally active, selective ghrelin (GHSR1a) receptor agonist developed for cancer anorexia-cachexia; approved in Japan for cachexia in several cancers.
Overview
Anamorelin is a small-molecule mimetic of the gut hormone ghrelin, the endogenous ligand of the growth-hormone secretagogue receptor (GHSR1a). By activating this receptor centrally and peripherally it stimulates appetite, drives a modest rise in growth hormone and IGF-1, and promotes an anabolic state that counteracts the muscle and weight loss of cancer cachexia.
In the pivotal ROMANA 1 and ROMANA 2 phase 3 trials in advanced non-small-cell lung cancer, anamorelin 100 mg once daily significantly increased lean body mass and improved anorexia-cachexia symptoms compared with placebo over 12 weeks, although the co-primary endpoint of handgrip strength was not met. The ROMANA 3 safety extension confirmed durable benefits and good tolerability out to 24 weeks.
The most common drug-related adverse effect is hyperglycaemia, reflecting ghrelin's role in glucose metabolism. Anamorelin remains investigational in the United States and Europe but is an approved therapy in Japan.
Mechanism of Action
Ghrelin receptor activation couples through Gq signalling in hypothalamic neurons to increase food intake and through the pituitary to release growth hormone, raising circulating IGF-1. The combined orexigenic and anabolic actions increase lean body mass and body weight. Because ghrelin also influences insulin secretion and glucose handling, hyperglycaemia is the principal metabolic side effect.
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References (2)
- [1]Temel JS, Abernethy AP, Currow DC, et al. Anamorelin in patients with non-small-cell lung cancer and cachexia (ROMANA 1 and ROMANA 2): results from two randomised, double-blind, phase 3 trials The Lancet Oncology (2016)
→ Anamorelin 100 mg once daily significantly increased lean body mass versus placebo over 12 weeks in advanced NSCLC patients with cachexia, though handgrip strength did not improve.
- [2]Currow D, Temel JS, Abernethy A, et al. ROMANA 3: a phase 3 safety extension study of anamorelin in advanced non-small-cell lung cancer (NSCLC) patients with cachexia Annals of Oncology (2017)
→ Extended dosing to 24 weeks was well tolerated and maintained body-weight and anorexia-cachexia symptom benefits, with hyperglycaemia the most common drug-related adverse event.
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