Tirzepatide

Description
Sources: https://pubmed.ncbi.nlm.nih.gov/35830001|https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=d2d7da5d-ad07-4228-955f-cf7e355c8cc0&type=display|https://www.ncbi.nlm.nih.gov/books/NBK585056/

Tirzepatide (Mounjaro™) is a single molecule that combines dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Tirzepatide is a GIP receptor and GLP-1 receptor agonist. It is a 39-amino-acid modified peptide with a C20 fatty diacid moiety that enables albumin binding and prolongs the half-life. Tirzepatide selectively binds to and activates both the GIP and GLP-1 receptors, the targets for native GIP and GLP-1. Tirzepatide enhances first- and second-phase insulin secretion, and reduces glucagon levels, both in a glucose-dependent manner. GIP also plays a role in nutrient and energy metabolism, while GLP-1 also delays gastric emptying, supresses appetite and improves satiety. Eli Lilly is developing tirzepatide for the treatment of type 2 diabetes mellitus (T2DM), obesity, cardiovascular disorders in T2DM, heart failure, non-alcoholic steatohepatitis, obstructive sleep apnoea and for reducing mortality/morbidity in obesity. In May 2022, tirzepatide received its first approval in the USA to improve glycaemic control in adults with T2DM, as an adjunct to diet and exercise. Tirzepatide is in phase III development for heart failure, obesity and cardiovascular disorders in T2DM, and in phase II development for non-alcoholic steatohepatitis. Tirzepatide can also be used off-label for treating obesity. It is currently implemented as a second-line diabetes medication, similar to GLP-1 medications like semaglutide. It is a once-a-week subcutaneous injectable medication with incremental dose increases.

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Gastric inhibitory polypeptide receptor 1 Target ID: CHEMBL4383 Sources: https://pubmed.ncbi.nlm.nih.gov/32730231\|https://pubmed.ncbi.nlm.nih.gov/30473097\|https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=d2d7da5d-ad07-4228-955f-cf7e355c8cc0&type=display	Agonist 2752		0.135 nM [Ki]
Glucagon-like peptide 1 receptor 5 Target ID: CHEMBL1784 Sources: https://pubmed.ncbi.nlm.nih.gov/32730231\|https://pubmed.ncbi.nlm.nih.gov/30473097\|https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=d2d7da5d-ad07-4228-955f-cf7e355c8cc0&type=display	Agonist 2752		4.23 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=d2d7da5d-ad07-4228-955f-cf7e355c8cc0&type=display	Primary		Approved 8583	MOUNJARO Approved Use MOUNJARO™ is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Launch Date 2022

C_max

Value	Dose	Analyte	Population
664 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	5 mg 1 times / week steady-state, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1340 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	10 mg 1 times / week steady-state, subcutaneous dose: 10 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1990 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	15 mg 1 times / week steady-state, subcutaneous dose: 15 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
26 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.25 mg single, subcutaneous dose: 0.25 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
57.7 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.5 mg single, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
108 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	1 mg single, subcutaneous dose: 1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
231 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	2.5 mg single, subcutaneous dose: 2.5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
397 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	5 mg single, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
874 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	8 mg single, subcutaneous dose: 8 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
77.8 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.5 mg 1 times / week multiple, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
198 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	1.5 mg 1 times / week multiple, subcutaneous dose: 1.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
884 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	4.5 mg 1 times / week multiple, subcutaneous dose: 4.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1510 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
54.6 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	0.5 mg 1 times / week multiple, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
614 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1030 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1250 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1520 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	2.5 mg 1 times / week multiple, subcutaneous dose: 2.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2270 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
838 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
663 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=26	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1270 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=26	7.5 mg 1 times / week multiple, subcutaneous dose: 7.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1900 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=26	10 mg 1 times / week multiple, subcutaneous dose: 10 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
83300 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	5 mg 1 times / week steady-state, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
168000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	10 mg 1 times / week steady-state, subcutaneous dose: 10 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
250000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	15 mg 1 times / week steady-state, subcutaneous dose: 15 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5760 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.25 mg single, subcutaneous dose: 0.25 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
12000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.5 mg single, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
22600 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	1 mg single, subcutaneous dose: 1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
53200 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	2.5 mg single, subcutaneous dose: 2.5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
90500 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	5 mg single, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
169000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	8 mg single, subcutaneous dose: 8 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
10600 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.5 mg 1 times / week multiple, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
24800 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	1.5 mg 1 times / week multiple, subcutaneous dose: 1.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
103000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	4.5 mg 1 times / week multiple, subcutaneous dose: 4.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
198000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
7200 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	0.5 mg 1 times / week multiple, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
81900 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
131000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
164000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
192000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	2.5 mg 1 times / week multiple, subcutaneous dose: 2.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
285000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
104000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
68900 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=26	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
149000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=26	7.5 mg 1 times / week multiple, subcutaneous dose: 7.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
5 day OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=4 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=9	5 mg single, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
116 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.25 mg single, subcutaneous dose: 0.25 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
124 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.5 mg single, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
108 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	1 mg single, subcutaneous dose: 1 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
120 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	2.5 mg single, subcutaneous dose: 2.5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
123 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	5 mg single, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
111 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	8 mg single, subcutaneous dose: 8 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
152 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	0.5 mg 1 times / week multiple, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
113 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	1.5 mg 1 times / week multiple, subcutaneous dose: 1.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
132 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	4.5 mg 1 times / week multiple, subcutaneous dose: 4.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
126 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=19	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
120 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	0.5 mg 1 times / week multiple, subcutaneous dose: 0.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
114 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
115 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
104 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=20	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
135 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	2.5 mg 1 times / week multiple, subcutaneous dose: 2.5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
121 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
127 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=23	5 mg 1 times / week multiple, subcutaneous dose: 5 mg route of administration: Subcutaneous experiment type: MULTIPLE co-administered:	TIRZEPATIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.94% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000PharmR.pdf#page=28 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf#page=34			TIRZEPATIDE plasma	Homo sapiens

Doses

Dose	Population	Adverse events
15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	Disc. AE: Diarrhea, Nausea... AEs leading to discontinuation/dose reduction: Diarrhea (1.1%) Nausea (0.8%) Dyspepsia (0.6%) Abdominal discomfort (0.6%) Gastrointestinal disorder (1.4%) Blood calcitonin increased (0.3%) Colitis ischaemia (0.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf

AEs

AE	Significance	Dose	Population
Blood calcitonin increased	0.3% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf
Colitis ischaemia	0.3% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf
Abdominal discomfort	0.6% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf
Dyspepsia	0.6% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf
Nausea	0.8% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf
Diarrhea	1.1% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf
Gastrointestinal disorder	1.4% Disc. AE	15 mg 1 times / week multiple, subcutaneous Highest studied dose Dose: 15 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 15 mg, 1 times / week Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000MedR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inhibitor 2438 inducer 440	inducer 109 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2B6 926 OAT3 747 CYP2C8 1057 P-gp 1741 CYP3A 227 BCRP 910 OATP1B1 1079 OATP1B3 961 OCT1 620 OCT2 779 OAT1 725 CYP2C19 2057 MATE1 415 MATE2K 17		CYP2B6 669 CYP2C19 329 CYP2C8 198 CYP3A5 92 CYP1A2 832

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no [IC50 >100 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP2D6 2546	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
CYP3A5 201	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
MATE2K 17	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 35.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely [IC50 129.65 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000ClinPharmR.pdf Page: 36.0	unlikely

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/215866Orig1s000PharmR.pdf Page: 25.0

PubMed

Title	Date	PubMed
Tirzepatide: First Approval.	2022-07	35830001
Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist.	2020-09-03	32730231
LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.	2018-12	30473097

Patents

Sample Use Guides

In Vivo Use Guide

The recommended starting dosage is 2.5 mg injected subcutaneously once weekly (2.1) After 4 weeks, increase to 5 mg injected subcutaneously once weekly (2.1) If additional glycemic control is needed, increase the dosage in 2.5 mg increments after at least 4 weeks on the current dose. The maximum dosage is 15 mg subcutaneously once weekly (2.1). Administer once weekly at any time of day, with or without meals. (2.2) Inject subcutaneously in the abdomen, thigh, or upper arm. (2.2) Rotate injection sites with each dose.

Route of Administration: Subcutaneous

In Vitro Use Guide

In signaling studies using cell lines with recombinantly expressed GIPR or GLP-1R, LY3298176 potently stimulates cAMP accumulation by either receptor (GIPR EC50 = 0.0224, SEM = 0.0053 nM; GLP-1R EC50 = 0.934, SEM = 0.068 nM)

Substance Class	Protein Created by `admin` on `Tue Apr 01 20:37:04 GMT 2025` Edited by `admin` on `Tue Apr 01 20:37:04 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	OYN3CCI6QE
Record Status	`FAILED`
Record Version

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Name

Type

Language

Tirzepatide

Official Name

English

MOUNJARO

Preferred Name

English

LY3298176

Code

English

LY-3298176

Code

English

TIRZEPATIDE [USAN]

Common Name

English

L-Tyrosyl-2-methylalanyl-L-?-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-?-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methylalanyl-L-leucyl-L-?-aspartyl-L-lysyl-L-isoleucyl-L-alanyl-L-glutaminyl-N6-[(22S)-22,42-dicarboxy-1,10,19,24-tetrao

Systematic Name

English

L-Serinamide, L-tyrosyl-2-methylalanyl-L-?-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-?-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methylalanyl-L-leucyl-L-?-aspartyl-L-lysyl-L-isoleucyl-L-alanyl-L-glutaminyl-N6-[(22S)-22,42-dicarboxy-1,1

Systematic Name

English

TIRZEPATIDE [JAN]

Common Name

English

Tirzepatide [WHO-DD]

Common Name

English

tirzepatide [INN]

Common Name

English

BG-121

Code

English

ZEPBOUND

Brand Name

English

Code System Code Type Description

USAN

EF-81