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Tirzepatide

CHEMBL4297839 Phase 4 Đã phê duyệt Protein
Half-Life
5 days
Bioavailability
—
Protein Binding
—
Molecular Weight
4813.0 g/mol
LogP
-6.8
Phase
4

Tirzepatide is a first-in-class dual glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptor agonist (twincretin) that activates both incretin receptor systems to enhance glucose-dependent insulin secretion, suppress glucagon, slow gastric emptying, and reduce appetite through hypothalamic pathways. It is approved for type 2 diabetes and obesity, showing superior glycemic control and weight loss compared to GLP-1 receptor agonists alone, and is under investigation for heart failure with preserved ejection fraction, sleep apnea, and fatty liver disease. Its novel dual incretin action represents a significant advance in metabolic disease pharmacotherapy.

Khối lượng phân tử

4813,0000 g/mol

LogP

-6,80

TPSA

1790,00 Ų

Lipinski RO5

Không đạt

Lĩnh vực điều trị

Cardiovascular Disease Osteoporosis Schizophrenia Psoriasis Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Obesity Type 2 Diabetes Hypertension Breast Cancer HIV/AIDS Heart Failure Atrial Fibrillation Prostate Cancer Colorectal Cancer Leukemia

Phân loại thuốc

A — A - Alimentary Tract and Metabolism

Cơ chế tác dụng

Dual GIP and GLP-1 receptor agonist.

Pharmacokinetics (PK)

Half-Life 5 days

Pharmacodynamics (PD)

Cơ chế

Dual GIP and GLP-1 receptor agonist.

SMILES

CCC(C)C(C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)NC(C)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)NC(CCC(=O)N)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NC(CC(C)C)C(=O)NC(C(C)CC)C(=O)NC(C)C(=O)NCC(=O)NCC(=O)N4CCCC4C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N5CCCC5C(=O)N6CCCC6C(=O)N7CCCC7C(=O)NC(CO)C(=O)N)NC(=O)C(CCCCN)NC(=O)C(CC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(C)(C)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(CC8=CC=C(C=C8)O)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC9=CC=CC=C9)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(C)(C)NC(=O)C(CC1=CC=C(C=C1)O)N

InChI

InChI=1S/C225H348N48O68/c1-23-126(10)183(264-198(311)146(64-50-52-88-226)246-202(315)157(109-180(297)298)252-199(312)152(103-124(6)7)261-223(337)225(21,22)269-217(330)185(128(12)25-3)266-209(322)163(120-278)257-200(313)153(107-138-74-78-141(282)79-75-138)250-203(316)158(110-181(299)300)253-207(320)162(119-277)259-216(329)187(134(18)280)267-206(319)155(106-136-60-44-41-45-61-136)254-215(328)186(133(17)279)262-174(289)114-237-193(306)147(83-87-179(295)296)260-222(336)224(19,20)268-192(305)143(227)104-137-72-76-140(281)77-73-137)214(327)242-131(15)190(303)244-148(80-84-168(228)283)196(309)245-145(65-51-53-89-231-175(290)121-340-100-99-339-97-91-233-176(291)122-341-101-98-338-96-90-232-170(285)86-82-150(221(334)335)243-171(286)70-46-38-36-34-32-30-28-26-27-29-31-33-35-37-39-47-71-178(293)294)195(308)240-130(14)191(304)248-154(105-135-58-42-40-43-59-135)205(318)263-182(125(8)9)212(325)247-149(81-85-169(229)284)197(310)251-156(108-139-111-234-144-63-49-48-62-142(139)144)201(314)249-151(102-123(4)5)204(317)265-184(127(11)24-2)213(326)241-129(13)189(302)236-112-172(287)235-115-177(292)270-92-54-66-164(270)210(323)258-161(118-276)208(321)256-160(117-275)194(307)238-113-173(288)239-132(16)218(331)272-94-56-68-166(272)220(333)273-95-57-69-167(273)219(332)271-93-55-67-165(271)211(324)255-159(116-274)188(230)301/h40-45,48-49,58-63,72-79,111,123-134,143,145-167,182-187,234,274-282H,23-39,46-47,50-57,64-71,80-110,112-122,226-227H2,1-22H3,(H2,228,283)(H2,229,284)(H2,230,301)(H,231,290)(H,232,285)(H,233,291)(H,235,287)(H,236,302)(H,237,306)(H,238,307)(H,239,288)(H,240,308)(H,241,326)(H,242,327)(H,243,286)(H,244,303)(H,245,309)(H,246,315)(H,247,325)(H,248,304)(H,249,314)(H,250,316)(H,251,310)(H,252,312)(H,253,320)(H,254,328)(H,255,324)(H,256,321)(H,257,313)(H,258,323)(H,259,329)(H,260,336)(H,261,337)(H,262,289)(H,263,318)(H,264,311)(H,265,317)(H,266,322)(H,267,319)(H,268,305)(H,269,330)(H,293,294)(H,295,296)(H,297,298)(H,299,300)(H,334,335)

Molecular Formula

C225H348N48O68

HBD / HBA

58 / 70

Liên kết có thể quay

163

Nguyên tử nặng

341

PPARG (Peroxisome Proliferator-Activated Receptor Gamma) Agonist
Primary Target
Moderate Tirzepatide + Sitagliptin

Combining tirzepatide (dual GIP/GLP-1 agonist) with sitagliptin (DPP-4 inhibitor) produces overlapping incretin-based mechanisms with additive hypoglycaemia risk and no meaningful additional benefit over either agent alone.

No side effects recorded

Side effect data is not yet available for this drug.

Câu hỏi thường gặp

Tirzepatide is a first-in-class dual glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptor agonist (twincretin) that activates both incretin receptor systems to enhance glucose-dependent insulin secretion, suppress glucagon, slow gastric emptying, and reduce appetite through hypothalamic pathways. It is approved for type 2 diabetes and obesity, showing superior glycemic control and weight loss compared to GLP-1 receptor agonists alone, and is under investigation for heart failure with preserved ejection fraction, sleep apnea, and fatty liver disease. Its novel dual incretin action …

Dual GIP and GLP-1 receptor agonist.

Key pharmacokinetic parameters for Tirzepatide: Half-life: 5 days.

Yes, Tirzepatide is an approved drug. It has reached clinical phase 4. It is classified as a Protein.

ADME Journey →

Related Drugs

Same Drug Class

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{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

  • ChEMBL — European Bioinformatics Institute (EBI). CHEMBL4297839. Open-access bioactivity database.
  • PubChem — National Center for Biotechnology Information (NCBI). CID 168009818. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.

Tuyên bố miễn trách y tế

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.