Evidence reference only. Not medical advice, not a dosing guide, and not a recommendation to use any drug.
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LY3537021

MARKETED

selective GIPR agonist

5
graded findings
5
effect domains
Evidence spread
High evidence 0Moderate evidence 0Low evidence 5Very low evidence 0

LY3537021 is shown as a marketed evidence record where applicable. Findings describe observed research and regulatory records; they do not provide treatment advice.

Thin or bounded evidence here means uncertainty remains visible. It is not evidence that an effect has been ruled out.
LY3537021 MARKETED
Appetite and food intake Decrease
Low evidence

The selective GIPR agonist LY3537021 produced dose-dependent weight loss in phase 1 whose apparent mode of action is appetite suppression, inferred from spontaneous...

Long-acting GIPR agonist LY3537021 reduces body weight and fasting glucose in T2D: precli... Source
Full findingThe selective GIPR agonist LY3537021 produced dose-dependent weight loss in phase 1 whose apparent mode of action is appetite suppression, inferred from spontaneous adverse events of decreased appetite/early satiety; the formal appetite VAS showed no conclusive effect and energy intake was not formally measured.
PopulationPhase 1 (incl. T2D MAD), humans
Fundingindustry - Eli Lilly (trial sponsor; inferred from registration trial)
Scope limitsSponsor-authored (all-Lilly); COI-flag. Reused from corpus T9-GIPR-03. Only selective-GIPR-agonist human appetite readout; mechanism INFERRED from AEs, VAS inconclusive (not measured-positive).
Comparatorsplacebo
Thin or bounded evidence here means uncertainty remains visible. It is not evidence that an effect has been ruled out.
LY3537021 MARKETED
Glycaemic control Mixed
Low evidence

Transient reductions in fasting glucose in T2D participants that were not sustained vs placebo by day 29.

Long-acting GIPR agonist LY3537021 reduces body weight and fasting glucose in T2D: precli... Source
PopulationPhase 1 MAD, T2D participants (NCT04586907); placebo comparator
Fundingindustry - Eli Lilly (trial sponsor; inferred from registration trial)
Scope limitsGlycaemic benefit of selective GIPR agonism appears weaker/less durable than its weight effect in this short study — recorded neutrally.
Comparatorsplacebo
Thin or bounded evidence here means uncertainty remains visible. It is not evidence that an effect has been ruled out.
LY3537021 MARKETED
Pharmacology and mechanism Not directional
Low evidence

In-vitro potency greater than native GIP, GIPR-selective; half-life ~12 days supporting once-weekly dosing; no delay in gastric emptying after single SC dose.

Long-acting GIPR agonist LY3537021 reduces body weight and fasting glucose in T2D: precli... Source
PopulationIn vitro, rats, phase 1 humans
Fundingindustry - Eli Lilly (trial sponsor; inferred from registration trial)
Scope limitsLack of gastric-emptying delay distinguishes GIPR agonism mechanistically from GLP-1R agonism.
Comparatorsnative GIP; placebo
Thin or bounded evidence here means uncertainty remains visible. It is not evidence that an effect has been ruled out.
LY3537021 MARKETED
Gastrointestinal tolerability No change
Low evidence

Well tolerated with infrequent gastrointestinal adverse events.

Long-acting GIPR agonist LY3537021 reduces body weight and fasting glucose in T2D: precli... Source
PopulationPhase 1 SAD/MAD N=85; placebo comparator
Fundingindustry - Eli Lilly (trial sponsor; inferred from registration trial)
Scope limitsA separate Knop et al 2024 (Diabetes Obes Metab, DOI 10.1111/dom.15875) reported that adding a long-acting GIPR agonist improved GI tolerability of GLP-1RA therapy — consistent theme that GIPR agonism may be GI-sparing.
Comparatorsplacebo
Thin or bounded evidence here means uncertainty remains visible. It is not evidence that an effect has been ruled out.
LY3537021 MARKETED
Weight change Decrease
Low evidence

Selective GIPR agonist monotherapy induced dose-dependent body-weight reduction in a phase 1 MAD study, persisting after last dose.

Long-acting GIPR agonist LY3537021 reduces body weight and fasting glucose in T2D: precli... Source
PopulationPhase 1 SAD/MAD RCT (NCT04586907), Singapore; N=85 (SAD n=47, MAD n=38) healthy + T2D; baseline BMI 25.9-27.0; placebo comparator
Fundingindustry - Eli Lilly (trial sponsor; inferred from registration trial)
Scope limitsKey evidence that SELECTIVE GIPR AGONISM alone causes weight loss in humans — supports a distinct GIP-agonism contribution to multi-agonists (counterpoint to MariTide's GIPR-antagonist approach). Early phase, modest N, lean-ish baseline BMI; authors note need for overweight/obese cohorts.
Comparatorsplacebo