RECORDED OBSERVATION (why explicitly open): Two clinically active obesity agents act in OPPOSITE directions on the GIP receptor yet both produce substantial weight...
Tirzepatide
MARKETEDGIP/GLP-1 dual agonist
Tirzepatide is shown as a marketed evidence record where applicable. Findings describe observed research and regulatory records; they do not provide treatment advice.
Tirzepatide is injected subcutaneously once weekly into the abdomen, thigh or upper arm with site rotation, at any time of day with or without meals, and into a...
A missed tirzepatide dose may be taken within 4 days (96 h); otherwise skip it. The dosing day may be changed if at least 3 days separate doses.
Tirzepatide delays gastric emptying and may alter absorption of co-administered oral drugs; the EU SmPC advises monitoring narrow-therapeutic-index drugs (e.g....
Co-administration of tirzepatide with another tirzepatide-containing product or any GLP-1 receptor agonist is not recommended.
When tirzepatide is combined with insulin or a sulfonylurea, reducing the secretagogue/insulin dose (stepwise for insulin) lowers hypoglycaemia risk.
A first tirzepatide (Zepbound) dose transiently reduced paracetamol/acetaminophen peak concentration by ~55% and delayed tmax, resolving by week 6 on continued dosing;...
Zepbound maintenance dosing differs by indication, with obstructive sleep apnoea requiring 10 mg or 15 mg once weekly.
Tirzepatide starts at 2.5 mg once weekly, increases to 5 mg after 4 weeks, then in 2.5 mg steps at no less than 4-week intervals up to a 15 mg maximum (10 mg max in...
The absolute bioavailability of subcutaneous tirzepatide is 80%.
Tirzepatide metabolites are excreted via urine and faeces, with no intact tirzepatide observed in urine or faeces.
Tirzepatide has an elimination half-life of about 5 days (5-6 days for Zepbound populations), the basis for once-weekly dosing.
Tirzepatide is cleared by metabolism via proteolytic cleavage of the peptide backbone, beta-oxidation of its C20 fatty diacid and amide hydrolysis.
Steady-state tirzepatide concentrations are reached after about 4 weeks of once-weekly dosing.
Tirzepatide has a small apparent steady-state volume of distribution (~10 L) and is ~99% albumin-bound.
Tirzepatide is a once-weekly subcutaneous dual agonist of the GIP and GLP-1 receptors (39-amino-acid acylated peptide). Marketed (Mounjaro for T2D; Zepbound for...
Dose-headroom confound (competing hypothesis): the FDA Mounjaro Clinical Pharmacology FG/HbA1c Emax model shows tirzepatide's marketed doses reach only 74-89% of the...
FDA Zepbound Clinical Pharmacology review characterises tirzepatide as having GIPR activity similar to native GIP but GLP-1R activity lower than native GLP-1, and as a...
The EMA Mounjaro EPAR quantifies tirzepatide's potency at the human glucagon receptor (GCGR) as a cAMP functional EC50 of ~2350 nM - some three orders of magnitude...
Tirzepatide is contraindicated in the US for personal/family history of MTC or MEN 2 (also a boxed warning) and serious hypersensitivity; the EU contraindication is...
About half of Mounjaro-treated patients developed anti-tirzepatide antibodies, with low neutralising-antibody rates and no identified clinical impact.
In Zepbound trials the majority of patients developed anti-tirzepatide antibodies; neutralising antibodies were uncommon in the weight-management pool (2.7-2.8%) and...
Tirzepatide may reduce ORAL hormonal contraceptive efficacy via delayed gastric emptying; US labelling advises switching to a non-oral method or adding a barrier...
FDA boxed warning: in a 2-year rat study tirzepatide caused dose- and treatment-duration-dependent thyroid C-cell tumours at clinically relevant exposures;...
In a CV-outcomes meta-analysis, GLP-1 RAs increased gallbladder disorders by 26% but showed no difference in pancreatitis or neoplasm.
Composite gallbladder/biliary disease significantly associated with tirzepatide; pancreatitis and individual biliary endpoints NOT significantly increased.
Post hoc pooled analysis of SURMOUNT-1/-2/-3 (RCT data): no clinically meaningful PHQ-9 difference vs placebo over 72 weeks; suicidal ideation/behaviour (C-SSRS) low...
In a network meta-analysis, tirzepatide produced the greatest reduction in both fat mass and (absolute) lean body mass.
Withdrawing tirzepatide after a 36-week lead-in led to substantial weight REGAIN, whereas continued treatment maintained/augmented loss (randomized-withdrawal design).
In a post hoc analysis of the SURMOUNT-1 obesity RCT, tirzepatide lowered serum uric acid dose-dependently versus placebo over 72 weeks, with the effect independent of...
A mediation analysis in the same SURMOUNT-1 post hoc found that about 73% of tirzepatide's serum-uric-acid reduction was explained by weight loss - implicating weight...
Real-world data associate tirzepatide with higher osteoporosis/fragility-fracture risk than other GLP-1 RAs - a greatest-weight-loss/dual-agonist signal.
Anaesthesia narrative reviews: GLP-1 RAs and tirzepatide delay gastric emptying and raise aspiration considerations; data preliminary/conflicting; gastric ultrasound...
Tirzepatide has no established link to elevated ferritin per trial data and the SmPC, and no known direct effect on iron metabolism; elevated ferritin observed in...
The EU SmPC states tirzepatide could be considered for use during breast-feeding.
A human lactation study (n=11) after a single 5 mg dose found tirzepatide largely undetectable in breast milk (cumulative <0.02% of the maternal dose); US labels make...
Animal reproduction studies show malformations and growth reductions in rat and rabbit at sub-clinical exposures; the label states human data are insufficient, and for...
No overall differences in safety or efficacy were detected in elderly patients, with limited data above 75 years.
US labelling specifies no dose adjustment for hepatic impairment (no PK change across degrees of impairment).
Paediatric status differs by product/region: the US Mounjaro label establishes use in T2D from age 10 (with higher vomiting/abdominal pain/hypoglycaemia than adults);...
US labelling specifies no dose adjustment for renal impairment including ESRD, with advice to monitor renal function when initiating/escalating in patients with severe...
A single small phase-2 RCT (n=24, 12 weeks) found tirzepatide added to insulin in obese type-1 diabetes produced large weight loss (-8.7kg, 8.8%), a borderline HbA1c...
In obese men with metabolic hypogonadism, tirzepatide improved erectile function and raised testosterone, outperforming testosterone replacement on axis recovery.
Tirzepatide was associated with lower incident erectile dysfunction than several comparators in T2D men.
In premenopausal women with obesity, 24 weeks of tirzepatide increased the proportion of participants with cold-stimulated PET/CT-detectable brown adipose tissue (BAT)...
Phase 1 human study with whole-room indirect calorimetry: tirzepatide did NOT attenuate weight-loss-induced metabolic adaptation (no detectable preservation of...
FDA Mounjaro Pharm/Tox review (rodent lead): in diet-induced-obese mice tirzepatide raised metabolic rate more than semaglutide and, at pair-fed/body-weight-matched...
Design/rationale paper for the TABFAT trial: investigator-initiated RCT evaluating tirzepatide effects on BAT volume/activity (18F-FDG-PET/CT, MRI, infrared...
In high-fat-diet obese mice with a pair-fed control arm, tirzepatide exerted distinct effects on brown adipose tissue relative to white: significantly boosting BAT...
In HFD-obese mice and in 3T3-L1 adipocytes, tirzepatide promoted browning of white adipose tissue via the cAMP-PGC-1alpha-UCP1 signalling axis, reducing intracellular...
In male mice, intracerebroventricular (i.c.v.) tirzepatide reduced body weight and fat content vs pair-fed controls by increasing white adipose lipolysis and enhancing...
In a mouse model of postmenopausal metabolic dysfunction (obese-diabetic +/- ovariectomy), tirzepatide reversed BAT 'whitening', restored multilocular brown adipocyte...
DIRECT head-to-head CVOT (SURPASS-CVOT, T2D + ASCVD). Tirzepatide (up to 15 mg) was NON-INFERIOR to dulaglutide 1.5 mg for 3-point MACE (~12% vs ~13%; HR 0.92, p=0.003...
DIRECT head-to-head (SURPASS-2, T2D). Tirzepatide at all three doses (5/10/15 mg) was non-inferior AND superior to semaglutide 1 mg for HbA1c reduction at 40 weeks;...
DIRECT head-to-head (SURMOUNT-5, obesity without T2D). Tirzepatide (max tolerated 10 or 15 mg) was SUPERIOR to semaglutide (max tolerated 1.7 or 2.4 mg) for weight...
DIRECT head-to-head post hoc (SURPASS-2). Tirzepatide improved attainment of composite therapeutic targets vs semaglutide 1 mg at 40 weeks. For standard targets, >=3...
INDIRECT (network meta-analysis, T2D). Across 76 RCTs / 15 GLP-1RA drugs / 39,246 participants, tirzepatide induced the LARGEST HbA1c reduction vs placebo (-2.10 pp,...
REAL-WORLD comparative effectiveness (Truveta EHR, overweight/obesity). Tirzepatide associated with significantly greater on-treatment weight loss than semaglutide...
REAL-WORLD comparative effectiveness (US clinical practice, obesity WITHOUT diabetes). At 6 months tirzepatide -11.15% vs semaglutide -8.83% (adjusted difference -2.32...
In T2D with established ASCVD, tirzepatide was NON-INFERIOR to dulaglutide for 3-point MACE but did NOT meet superiority. The comparator is a CV-proven GLP-1RA, so...
Pre-specified pre-registration pooled CV meta-analysis of the SURPASS phase-3 programme found tirzepatide did NOT increase MACE versus controls; the point estimate was...
Dedicated morbidity-mortality OUTCOME trial of tirzepatide in OBESITY WITHOUT diabetes (primary and secondary prevention) is ONGOING with no results; the first...
SURPASS-4 post hoc: tirzepatide slowed eGFR decline, prevented UACR rise and reduced a composite kidney endpoint versus insulin glargine.
SURPASS-CVOT prespecified exploratory: tirzepatide reduced major kidney events versus dulaglutide (direct incretin head-to-head).
In T2D with established ASCVD, tirzepatide reduced a composite of major adverse kidney events versus dulaglutide in a prespecified exploratory analysis of...
SURMOUNT-1 DXA substudy: tirzepatide's large total loss was accompanied by a PROPORTIONALLY matched lean loss (~25% of weight lost), and crucially the same ~75/25...
SUMMIT CMR substudy (obesity-related HFpEF): tirzepatide reduced LV mass and paracardiac (epicardial + pericardial) adipose tissue vs placebo at 52 weeks; the...
EHR-linked body-composition digital-phenotyping study (LLM extraction) of routine-care users found tirzepatide associated with GREATER relative lean-body-mass loss...
The FDA approved tirzepatide (Zepbound) in December 2024 for moderate-to-severe obstructive sleep apnoea in adults with obesity - the first-ever drug indication for...
In SURMOUNT-OSA trial 1 (APNEA-1, participants NOT on positive airway pressure), tirzepatide at max-tolerated dose (10/15 mg) markedly reduced the apnoea-hypopnoea...
In SURMOUNT-OSA trial 2 (APNEA-2, participants ON positive airway pressure), tirzepatide at max-tolerated dose (10/15 mg) markedly reduced the AHI vs placebo over 52...
SUMMIT: in HFpEF with obesity, tirzepatide reduced the composite of CV death or worsening HF event and improved KCCQ-CSS versus placebo.
In a mechanistic secondary analysis of SUMMIT, tirzepatide at 52 weeks reduced systolic blood pressure (-5 mmHg), estimated blood volume (-0.58 L), CRP (-37.2%),...
Tirzepatide dose-dependently improves the atherogenic lipoprotein profile: lowers TG, VLDL-C, ApoB, ApoC-III and small LDL particles; ApoC-III reduction partly...
In a post-hoc analysis of the phase-3 SURMOUNT-1 obesity trial, tirzepatide-associated improvements in triglycerides, HDL-C, LDL-C and non-HDL cholesterol were...
Tirzepatide reduces food cravings (Food Craving Inventory) and food-cue reward-circuit reactivity (fMRI) - the strongest MECHANISTIC evidence for the lay 'food noise'...
In a phase 1 mechanism-of-action trial in people with obesity (NCT04081337), tirzepatide reduced appetite and reduced calorie intake during an ad-libitum test meal vs...
In an INDEPENDENT (non-manufacturer) US lifetime microsimulation, tirzepatide and semaglutide added to lifestyle modification produced the largest QALY gains among...
In two large US claims/EHR databases, most adults WITHOUT type 2 diabetes who initiated tirzepatide were still persistent at 6 months - a higher 6-month persistence...
SURMOUNT-4 randomised-withdrawal RCT: after a 36-week open-label lead-in (mean loss 20.9%), participants were randomised at week 36 to continue tirzepatide or switch...
SURMOUNT-4 post-hoc: cardiometabolic markers tracked WITH the magnitude of weight regain after tirzepatide withdrawal - greater regain was associated with larger...
Tirzepatide reduced 24-hour ambulatory systolic BP versus placebo (SURMOUNT-1 ABPM substudy); effect partly weight-mediated.
Tirzepatide raises heart rate modestly and dose-dependently versus placebo.
GI AEs most common, mostly mild-to-moderate, primarily during dose escalation; AE-related discontinuation dose-related. Per-symptom rates broadly dose-related (nausea...
In SURPASS-2, all three tirzepatide doses were non-inferior and superior to semaglutide 1 mg for HbA1c reduction from baseline at 40 weeks (head-to-head).
In a single-arm 12-week clamp study (obese T2D, tirzepatide up to 5 mg) the glucose infusion rate rose and glucagon fell, with no significant correlation between GIR...
In SYNERGY-NASH (phase 2, F2-F3), the GIP/GLP-1 dual tirzepatide was superior to placebo for MASH resolution without fibrosis worsening at 52 wk across all doses. The...