Peginesatide
Peginesatide was a synthetic, PEGylated dimeric peptide that activated the EPO receptor despite having no sequence homology to erythropoietin. Approved in the US in 2012 for dialysis anaemia, it was withdrawn in 2013 after fatal anaphylaxis reports. Because it evaded EPO immunoassays, it drew anti-doping concern. Prohibited by WADA as an EPO-receptor agonist.
01 Overview
Peginesatide (Omontys) was a peptide-based ESA: two short synthetic peptides linked and PEGylated, agonising the EPO receptor with structure entirely unlike natural EPO. It offered monthly dosing for haemodialysis patients.\n\nWithin a year of launch it was voluntarily recalled and withdrawn after post-marketing reports of serious hypersensitivity, including fatal anaphylactic reactions occurring mostly on first exposure. Its structural novelty meant standard EPO detection methods did not catch it, which is precisely why anti-doping bodies flagged it; dedicated assays were subsequently described. It is no longer marketed.
02 Mechanism
A synthetic PEGylated peptide dimer that binds and activates the erythropoietin receptor without any structural relationship to native EPO, triggering the same downstream erythropoietic signalling.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Dialysis anaemia (former) | 0.04–0.08 mg/kg | IV | Monthly; product withdrawn 2013 |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Erythropoiesis with monthly dosingMaintained haemoglobin in dialysis patients with once-monthly injection before withdrawal. | Hb maintained | Clinical | |
| Evaded standard EPO immunoassaysIts non-EPO-like structure meant conventional EPO detection missed it, the source of anti-doping concern; dedicated assays were later developed. | Distinct structure | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Anaphylaxis / severe hypersensitivityPost-marketing fatal anaphylactic reactions, typically on first exposure, prompted global withdrawal in 2013. | Life-threatening | Rare but fatal, led to withdrawal | Clinical | |
| ThromboembolismShared ESA clotting risk from raised haematocrit. | Severe | ESA-class risk | Clinical |