Anamorelin (Adlumiz)
Orally active small-molecule ghrelin receptor agonist approved in Japan for cancer-associated cachexia.
At a glance
What it is: Orally active small-molecule ghrelin receptor agonist approved in Japan for cancer-associated cachexia..
Primary research applications:
- Cancer-associated cachexia
- Anorexia and weight loss in chronic disease (research)
Editorial summary: Anamorelin is the closest the field has come to a marketed ghrelin-mimetic for cancer cachexia. It received approval in Japan as Adlumiz in 2021 for non-small-cell lung cancer cachexia, but did not receive approval in the EU or US — an instructive case in how regulatory standards differ across jurisdictions for cachexia indications. Like MK-677, it is technically a small molecule rather than a peptide, but is discussed alongside the peptide GH secretagogues.
- Class / structure
- Synthetic small molecule (not a peptide); ghrelin/GHS-R agonist
- Half-life
- ≈ 7 hours (oral)
- First described
- Late 2000s (Helsinn Healthcare)
- Regulatory status
- Approved in Japan (2021 — Adlumiz, NSCLC cachexia); not approved in US/EU
What is Anamorelin?
Anamorelin is a small-molecule ghrelin/GHS-R agonist that mimics the action of ghrelin on appetite, growth hormone secretion, and adipose-tissue signaling.
Discovery and development
Anamorelin was developed by Helsinn Healthcare as an orally active ghrelin/GHS-R agonist with a focused indication strategy: cancer-associated cachexia, where stimulating appetite and lean-mass preservation could meaningfully address an unmet medical need. The Phase 3 ROMANA-1 and ROMANA-2 trials supported approval in Japan as Adlumiz in 2021 for cachexia in non-small-cell lung cancer; the EMA and FDA declined approval, citing concerns about the magnitude of clinically meaningful effect.
Mechanism of action
GHS-R activation drives appetite stimulation via central pathways and produces pulsatile growth hormone release. The clinical rationale in cachexia combines appetite stimulation, lean-mass support via GH/IGF-1 elevation, and direct effects on adipose tissue.[1]
Pharmacokinetics
Oral once-daily dosing. Half-life of approximately seven hours supports daily administration; food does not meaningfully alter absorption.
What the research shows
The peer-reviewed literature on Anamorelin is summarized below across two tiers: human research (the highest standard), and preclinical / emerging research (animal models and early-stage human work).
Claims and the evidence behind them
This table summarizes commonly discussed claims and how the published evidence weighs in. The aim is clarity — supported claims, claims that look promising but need more data, and claims that outrun the science.
| Claim | What the evidence shows | Verdict |
|---|---|---|
| Increases lean body mass and weight in cancer cachexia | ROMANA trials | Supported |
| Improves handgrip strength as a functional outcome | ROMANA trials did not show this | Unsupported |
| Approved in the US or EU | FDA and EMA declined approval | Unsupported |
| Approved in Japan for NSCLC cachexia | Adlumiz approved 2021 | Supported |
Reported user experiences
How the research describes administration
Oral once-daily dosing under specialist supervision in cachexia management. Available only in Japan as a marketed product; outside Japan, used in research contexts.
Editorial note
Administration details above describe how the peptide is given in published studies. We summarize this for educational completeness — these descriptions are not protocols, dosing recommendations, or instructions for personal use. Decisions about treatment require an appropriately licensed clinician.
Safety considerations and open questions
The takeaway
Anamorelin is the most clinically advanced ghrelin-mimetic ever developed — and its mixed regulatory outcome illustrates how cachexia indications require demonstrating both anabolic and functional improvement. It remains a reference compound for the broader ghrelin/GH-secretagogue therapeutic concept, alongside MK-677 and the peptide GH secretagogues.
Frequently asked questions
Is anamorelin a peptide?
No. It is a small molecule that acts on the same receptor (GHS-R1a) as the peptide GH secretagogues. We cover it here because it is part of the broader ghrelin/GH-secretagogue therapeutic conversation.
Why didn't the FDA approve anamorelin?
The FDA and EMA cited the absence of functional improvement (handgrip strength) in the Phase 3 trials, despite increases in lean body mass and weight. The Japanese regulatory framework for cachexia weighed the data differently.
References
- Currow DC, et al. ROMANA 3: a phase 3 safety extension study of anamorelin in advanced non-small-cell lung cancer (NSCLC) patients with cachexia. Ann Oncol. 2017;28(8):1949-1956. https://pubmed.ncbi.nlm.nih.gov/28838212/
- Temel JS, et al. Anamorelin in patients with non-small-cell lung cancer and cachexia (ROMANA 1 and ROMANA 2). Lancet Oncol. 2016;17(4):519-531. https://pubmed.ncbi.nlm.nih.gov/26906526/