Tirzepatide: dosing, evidence and sources

Mechanism

Combines GLP-1 satiety/gastric-delay signaling with GIP insulinotropic effects.

Regulatory status

Approved by the FDA. Marketed as MOUNJARO, MOUNJARO KWIKPEN, ZEPBOUND, ZEPBOUND KWIKPEN. Earliest approval 2022-05-13. Application NDA215866, NDA217806.

An approval grades as rung 1 on this site, because 21 CFR 314.126 requires adequate and well-controlled human investigations and one cannot be granted without them. It covers specific indications and doses, though, and does not transfer to other uses of the same molecule.

Reported effects

What sources associate with this compound. Reported categories, not outcomes we have graded — each would need its own citation and rung.

Weight loss
Glycemic control
OSA improvement context

Dosing on file unverified

0.5-15 mg weekly, cycled 12–72 weeks

Reported dose	Volume	Draw
Low — 0.5 mg	0.2 mL	20 units
High — 15 mg	6 mL	600 units

What that assumes. Assumes 5 mg in 2 mL (2500 mcg/mL) drawn on a U-100 barrel — the preset on this record, not a recommendation and not the only way to mix it. Change the vial mass, the diluent or the barrel and every number in this table changes. Run your own.

Carried from a source that labels it unverified, and reproduced with that label attached. A record of what is reported, not a recommendation. No citation on this page establishes it.

Reconstitution

Vial	Diluent	Concentration	Typical dose	Draw
5 mg	2 mL	2500 mcg/mL	500 mcg	20 units

mass ÷ diluent = concentration; dose ÷ concentration = volume; volume × the syringe factor = units on the barrel (100 for U-100, 40 for U-40). Run your own numbers.

Reported adverse effects

Nausea

Very common (>10%)onset: Dose escalationreported reversible
Diarrhea

Common (1-10%)onset: First weeksreported reversible
Decreased appetite

Very common (>10%)onset: Ongoing — intended effectreported reversible
Vomiting

Common (1-10%)onset: Dose escalationreported reversible

Literature on file 5

human RCT
FDA approval NDA215866, NDA217806 graded on: an FDA approval (NDA215866, NDA217806), which requires adequate and well-controlled human investigations — “NDA215866, NDA217806”

Not graded

4 citations whose study design could not be read from the title. Left ungraded rather than guessed at.

Identity

Space-filling 3D model of Tirzepatide, carbon grey, nitrogen blue, oxygen red — Built from the SMILES on this record — the atoms, bonds and stereochemistry are exact. The shape is **one computed low-energy pose**, not a measured structure: a flexible peptide in solution has no single conformation. The skeletal formula below claims connectivity and nothing more, which is what we actually know.

2D chemical structure of Tirzepatide — Built from the SMILES on this record — the atoms, bonds and stereochemistry are exact. The shape is **one computed low-energy pose**, not a measured structure: a flexible peptide in solution has no single conformation. The skeletal formula below claims connectivity and nothing more, which is what we actually know.

Molecular weight: 4813
Molecular formula: C225H348N48O68
CAS number: 2023788-19-2
PubChem CID: 156588324; 168009818
UniProt: P43220 & P48546 (Targets)
ChEMBL: CHEMBL4297839
InChI key: AAPYRSPHYSKGIS-MCNPHUAVSA-N
SMILES: CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N4CCC[C@H]4C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N7CCC[C@H]7C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CCCCNC(=O)CCCCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)O)C(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)C(C)(C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CC8=CC=C(C=C8)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC9=CC=CC=C9)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@H](CC1=CC=C(C=C1)O)N
InChI: InChI=1S/C225H348N48O68/c1-23-126(10)183(214(327)242-131(15)190(303)244-148(80-84-168(228)283)196(309)245-145(64-50-52-88-226)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)236-112-173(288)235-115-177(292)270-92-54-66-164(270)210(323)258-161(118-276)208(321)256-160(117-275)194(307)238-113-174(289)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)264-198(311)146(65-51-53-89-231-170(285)70-46-38-36-34-32-30-28-26-27-29-31-33-35-37-39-47-71-172(287)243-150(221(334)335)82-86-171(286)232-90-96-338-98-100-340-121-176(291)233-91-97-339-99-101-341-122-181(299)300)246-202(315)157(109-179(295)296)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(110-180(297)298)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)262-175(290)114-237-193(306)147(83-87-178(293)294)260-222(336)224(19,20)268-192(305)143(227)104-137-72-76-140(281)77-73-137/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,231,285)(H,232,286)(H,233,291)(H,235,288)(H,236,302)(H,237,306)(H,238,307)(H,239,289)(H,240,308)(H,241,326)(H,242,327)(H,243,287)(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,262,290)(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)/t126-,127-,128-,129-,130-,131-,132-,133+,134+,143-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,159-,160-,161-,162-,163-,164-,165-,166-,167-,182-,183-,184-,185-,186-,187-/m0/s1

Classified as

Incretin Signalingpathway: Almost every compound sold as a GLP-1 acts somewhere on this pathway, and the real differences between them, one receptor or two, how long they last, how they are cleared, sit here rather than in the trade name.
Glucose Homeostasispathway: The readings a record may cite cover different windows: a fasting glucose is one moment, HbA1c reflects roughly the previous three months, a continuous monitor's average is neither. Comparing across them is a common error.
Subcutaneousroute: This is the route the reconstitution arithmetic assumes. Mass divided by diluent volume gives concentration, dose divided by concentration gives volume, and volume in mL multiplied by 100 gives units on a U-100 barrel: 5 mg in 2 mL is 2.5 mg/mL, and 0.25 mg comes out at 0.1 mL, which is 10 units.

Also called

Tirzepatide

Caveat on these identifiers

P43220 is the GLP-1 RECEPTOR, not the drug itself. P48546 is the GIP RECEPTOR, not the drug itself. PubChem record exists but is untitled; formula matches tirzepatide (CID 156588324).

Notes unverified prose

FDA-approved; SURMOUNT trials; SURMOUNT-MAINTAIN; PMID: 40353578; SURMOUNT-OSA; PMID: 39378016

Not on file 1

1 of the 8 fields we track hold nothing on this record, and each says why. A blank field is a bug; a named absence is a finding.

amino-acid sequenceno source on file holds this

Each field links to every other record missing the same thing. The full ledger holds 521 gaps across 136 records.