Tirzepatide

Summary

Tirzepatide (CHEMBL4297839) is an approved protein (ATC A10BX16) targeting GIPR and GLP1R; indicated across 8 conditions including obesity disorder and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: A10BX16
• Targets: 2 (GIPR, GLP1R)
• Indications: 8 conditions
• Clinical trials: 188

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297839
Name	Tirzepatide
Type	Protein
Max phase	4
ATC	A10BX16

Also known as: BG-121, LY-3298176, Ly3298176, LY3298176, Mounjaro, Mounjaro (autoinjector), Tirzepatida, Tirzepatide, Zepbound, Zepbound (autoinjector), TIRZEPATIDE

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GIPR	GIP receptor	Agonist	9.87	0.2%	P48546
GLP1R	GLP-1 receptor	Agonist	8.37	0.2%	P43220

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Glucagon-like peptide 1 receptor, Gastric inhibitory polypeptide receptor.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GIPR	10.52	EC50	0.03	nM	CHEMBL_ACT_26005728
GLP1R	9.11	EC50	0.77	nM	CHEMBL_ACT_26005753

Target pathways

Aggregated over 2 target gene(s): GIPR, GLP1R.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
G alpha (s) signalling events	2	GIPR, GLP1R
Glucagon-type ligand receptors	2	GIPR, GLP1R
Glucagon-like Peptide-1 (GLP1) regulates insulin secretion	1	GLP1R

Dominant GO biological processes

GO term	Targets
cell surface receptor signaling pathway	2
adenylate cyclase-activating G protein-coupled receptor signaling pathway	2
activation of adenylate cyclase activity	2
positive regulation of cytosolic calcium ion concentration	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
desensitization of G protein-coupled receptor signaling pathway	1
generation of precursor metabolites and energy	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
response to nutrient	1
response to glucose	1
endocrine pancreas development	1
positive regulation of insulin secretion	1
gastric inhibitory peptide signaling pathway	1
response to axon injury	1

Indications & clinical

Indications

8 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
obesity disorder	4	MONDO:0011122	EFO:0001073
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148
diabetes mellitus	4	MONDO:0005015	EFO:0000400
metabolic dysfunction-associated steatohepatitis	2	MONDO:0007027	EFO:1001249
chronic kidney disease	2	MONDO:0005300	EFO:0003884
Wolfram syndrome	2	MONDO:0018105	MONDO:0018105
morbid obesity	2	MONDO:0005139	EFO:0001074

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 188.

Phase distribution

Phase	Trials
PHASE2	54
PHASE3	41
PHASE4	29
Not specified	27
PHASE1	26
EARLY_PHASE1	5
PHASE1/PHASE2	4
PHASE2/PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05433584	PHASE4	ACTIVE_NOT_RECRUITING	A Study of Tirzepatide Compared With Intensified Conventional Care in Adult Participants With Type 2 Diabetes
NCT05553093	PHASE4	RECRUITING	Effects of Tirzepatide and Insulin Glargine on Glucolipid Metabolism and Brain Function in Patients With Type 2 Diabetes
NCT05708859	PHASE4	RECRUITING	Effect of Tirzepatide on Progression of Coronary Atherosclerosis Using MDCT
NCT06191848	PHASE4	RECRUITING	Subcutaneous Tirzepatide Once-weekly in Patients With Obesity and Knee Osteoarthritis (STOP KNEE-OA)
NCT06606821	PHASE4	RECRUITING	The Effects of Tirzepatide in People With Overweight/Obesity and Coronary Artery Disease
NCT06657209	PHASE4	RECRUITING	Normal-weight Diabetes: Adipocyte-directed Therapy With Pioglitazone or Tirzepatide
NCT06721507	PHASE4	RECRUITING	2024 Tirzepatide-Bariatric Surgery
NCT06774079	PHASE4	RECRUITING	Glucagon-like Peptide-1 Receptor Agonist (GLP-1 RA) and Diet in Inflammatory Bowel Disease (IBD) Patients
NCT06801015	PHASE4	ACTIVE_NOT_RECRUITING	Effects of Long-Acting GLP-1 (Glucagon-like Peptide-1) or Dual Incretin (GLP-1 and GIP [Glucose-dependent Insulinotropic Peptide]) Modulation on Gastric Motor Functions
NCT06803888	PHASE4	ACTIVE_NOT_RECRUITING	Bariatric Surgery vs. Semaglutide vs. Tirzepatide
NCT06857942	PHASE4	RECRUITING	A Study to Investigate the Effectiveness of Tirzepatide (LY3298176) Following Initiation of Ixekizumab (LY2439821) in Participants With Moderate-to-Severe Plaque PsO and Obesity or Overweight in Clinical Practice (TOGETHER AMPLIFY-PsO)
NCT06861439	PHASE4	ACTIVE_NOT_RECRUITING	GLP-1s to Enhance Lasting Optimal Weight
NCT06864026	PHASE4	RECRUITING	A Study to Investigate Effectiveness of Tirzepatide Following Initiation of Ixekizumab in Participants With Active Psoriatic Arthritis and Overweight or Obesity in Clinical Practice (TOGETHER AMPLIFY-PsA)
NCT06901245	PHASE4	RECRUITING	Tirzepatide in PWS, HO and GNSO
NCT07096908	PHASE4	RECRUITING	Tirzepatide Use in People With Obesity and Type 1 Diabetes
NCT07154719	PHASE4	RECRUITING	GLP-1R Actions on Muscle and the Skeleton
NCT07191873	PHASE4	NOT_YET_RECRUITING	Tirzepatide in Idiopathic Intracranial Hypertension Trial
NCT07218445	PHASE4	RECRUITING	The Effect of Tirzepatide on Menopausal Vasomotor Symptoms and Biological Aging in Post-menopausal Women With Obesity
NCT07247084	PHASE4	RECRUITING	A Study of Tirzepatide (LY3298176) Compared With Standard of Care in Adult Participants With Obesity and Without Diabetes (SURMOUNT-REAL UK)
NCT07257484	PHASE4	NOT_YET_RECRUITING	Tirzepatide’s Role in Postmenopausal HR+ Breast Cancer Survivors
NCT07423247	PHASE4	RECRUITING	Tirzepatide (Spartina) in Obese Kidney Transplant Recipients
NCT07438444	PHASE4	RECRUITING	A Study of Tirzepatide (LY3298176) in Adult Participants in India With Either Type 2 Diabetes Mellitus or Obesity
NCT07483801	PHASE4	NOT_YET_RECRUITING	DECODE - Haemodynamic Effects Of Semaglutide and Tirzepatide - a Series of Pilot Studies
NCT07554638	PHASE4	NOT_YET_RECRUITING	Incretin Therapies in Obesity-related HFpEF
NCT07555730	PHASE4	NOT_YET_RECRUITING	AI-assisted Multi-domain Lifestyle Versus Tirzepatide for Weight Loss Maintenance in Adults With Type 2 Diabetes (AIM-MAINTAIN)
NCT05564039	PHASE4	COMPLETED	A Study of Tirzepatide (LY3298176) in Adult Participants With Type 2 Diabetes Switching From Dulaglutide (SURPASS-SWITCH)
NCT05706506	PHASE4	COMPLETED	A Study of Tirzepatide (LY3298176) in Adults With Type 2 Diabetes Switching From a GLP-1 RA (SURPASS-SWITCH-2)
NCT06009653	PHASE4	WITHDRAWN	Effects of Tirzepatide Plus Intensive Lifestyle Therapy on Body Weight and Metabolic Health in Latinos With Obesity
NCT06635057	PHASE4	COMPLETED	A Study of Tirzepatide (LY3298176) in Participants With Type 2 Diabetes During Ramadan
NCT05556512	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Tirzepatide (LY3298176) on the Reduction on Morbidity and Mortality in Adults With Obesity
NCT06075667	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Tirzepatide (LY3298176) Once Weekly in Adolescent Participants Who Have Obesity or Overweight With Weight-Related Comorbidities
NCT06162715	PHASE2/PHASE3	ENROLLING_BY_INVITATION	GLP-1 Receptor Agonists Post-Bariatric Surgery (GRABS) Pilot Trial
NCT06246799	PHASE3	RECRUITING	Comparative Effectiveness of Two Initial Combination Therapies in Patients With Recent Onset Diabetes
NCT06439277	PHASE3	RECRUITING	A Study of Tirzepatide in Adolescents With Obesity and Weight-Related Comorbidities (SURMOUNT-ADOLESCENTS-2)
NCT06534411	PHASE3	ACTIVE_NOT_RECRUITING	A Research Study to See How Much CagriSema Lowers Blood Sugar and Body Weight Compared to Tirzepatide in People With Type 2 Diabetes Treated With Metformin, SGLT2 Inhibitor or Both
NCT06588283	PHASE3	ACTIVE_NOT_RECRUITING	Ixekizumab Concomitantly Administered With Tirzepatide in Adults With Moderate-to-Severe Plaque Psoriasis and Obesity or Overweight
NCT06630585	PHASE3	RECRUITING	GIP/GLP-1RA as Adjunctive to Automated Insulin Delivery in Adults With Type 1 Diabetes
NCT06662383	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Retatrutide (LY3437943) Compared to Tirzepatide (LY3298176) in Adults Who Have Obesity
NCT06914895	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Tirzepatide (LY3298176) Compared With Placebo in Adults With Type 1 Diabetes and Obesity or Overweight
NCT06918405	PHASE3	ACTIVE_NOT_RECRUITING	Efficacy and Safety of Tirzepatide for Weight Management

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

234 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	GIPR, GLP1R
CANDESARTAN CILEXETIL	ChEMBL + PubChem	Phase 4 (approved)	GIPR
LIRAGLUTIDE	ChEMBL + PubChem	Phase 4 (approved)	GLP1R
ELAGOLIX	ChEMBL	Phase 4 (approved)	GLP1R
EXENATIDE	ChEMBL	Phase 4 (approved)	GLP1R
GLUCAGON	ChEMBL	Phase 4 (approved)	GLP1R
LOPERAMIDE	ChEMBL	Phase 4 (approved)	GLP1R
PERPHENAZINE	ChEMBL	Phase 4 (approved)	GLP1R
SECRETIN	ChEMBL	Phase 4 (approved)	GLP1R
SEMAGLUTIDE	ChEMBL	Phase 4 (approved)	GLP1R
TOLVAPTAN	ChEMBL	Phase 4 (approved)	GLP1R
ORFORGLIPRON	ChEMBL	Phase 3	GLP1R
COTADUTIDE	ChEMBL	Phase 2	GLP1R
DANUGLIPRON	ChEMBL	Phase 2	GLP1R
DEVAZEPIDE	ChEMBL	Phase 2	GLP1R
GLP-1	ChEMBL	Phase 2	GLP1R
LOTIGLIPRON	ChEMBL	Phase 2	GLP1R
MK-0893	ChEMBL	Phase 2	GIPR
PF-06291874	ChEMBL	Phase 2	GLP1R
Acetylcholine	PubChem	Approved	GIPR
Aclidinium Bromide	PubChem	Approved	GIPR
Acyclovir	PubChem	Approved	GIPR
Alendronic Acid	PubChem	Approved	GIPR
Allopurinol	PubChem	Approved	GIPR
Alogliptin	PubChem	Approved	GIPR
Alprazolam	PubChem	Approved	GIPR
Amiloride	PubChem	Approved	GIPR
Amitriptyline	PubChem	Approved	GIPR
Amlodipine	PubChem	Approved	GIPR
Amoxapine	PubChem	Approved	GIPR
Amoxicillin	PubChem	Approved	GIPR
Amphetamine	PubChem	Approved	GIPR
Apomorphine	PubChem	Approved	GIPR
Aripiprazole	PubChem	Approved	GIPR
Aspirin	PubChem	Approved	GIPR
Atorvastatin	PubChem	Approved	GIPR
Azathioprine	PubChem	Approved	GIPR
azithromycin, unspecified form	PubChem	Approved	GIPR
Baclofen	PubChem	Approved	GIPR
Beclomethasone	PubChem	Approved	GIPR
Beclomethasone Dipropionate	PubChem	Approved	GIPR
Benazepril	PubChem	Approved	GIPR
Bicalutamide	PubChem	Approved	GIPR
Bisoprolol	PubChem	Approved	GIPR
Bosentan	PubChem	Approved	GIPR
Bosutinib	PubChem	Approved	GIPR
Bromocriptine	PubChem	Approved	GIPR
Bumetanide	PubChem	Approved	GIPR
Bupropion	PubChem	Approved	GIPR
Caffeine	PubChem	Approved	GIPR
Candesartan	PubChem	Approved	GIPR
Carisoprodol	PubChem	Approved	GIPR
Carvedilol	PubChem	Approved	GIPR
Celecoxib	PubChem	Approved	GIPR
cephalexin	PubChem	Approved	GIPR
Cetirizine	PubChem	Approved	GIPR
chlorpheniramine	PubChem	Approved	GIPR
Chlorpromazine	PubChem	Approved	GIPR
cianidanol	PubChem	Approved	GIPR
Cimetidine	PubChem	Approved	GIPR