Peringatan Keamanan

There is limited information regarding the LD₅₀ and overdose of tirzepatide. In case of an overdosage, appropriate supportive treatment should be initiated with a sufficient amount of time for observation and treatment, as tirzepatide has a long half-life.^L41815

Tirzepatide

DB15171

biotech approved investigational

Deskripsi

Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Dual GIP/GLP-1 agonists gained increasing attention as new therapeutic agents for glycemic and weight control as they demonstrated better glucose control and weight loss compared to selective GLP-1 receptor agonists in preclinical and clinical trials.^A246260

Tirzepatide comprises a 39 amino acid linear synthetic peptide conjugated to a C20 fatty diacid moiety.^A246260 Its protein sequence was based on the sequence of endogenous GIP, and its pharmacological action on GLP-1 receptors is comparable to endogenous GIP; however, the long half-life of tirzepatide allows for once-weekly dosing.^A246265 Tirzepatide was approved by the FDA on May 13, 2022, under the brand name MOUNJARO by the FDA for the treatment of adults with type 2 diabetes, making it the first and only GIP and GLP-1 receptor agonist for this indication.^L41820 Later, it was approved under a different brand name ZEPBOUND on November 8, 2023, for the chronic weight management in adults with obesity or overweight with at least one weight-related condition.^L48766 On September 15, 2022, tirzepatide was also approved by the European Commission.^L44386

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life is approximately five days.[A246265,L41815]

Volume Distribusi Following subcutaneous administration, the mean steady-state volume of distribution was 9.5 L.[A246260] The mean apparent steady-state volume of distribution of tirzepatide following subcutaneous administration in patients with type 2 diabetes mellitus was approximately 10.3 L.[L41815]

Klirens (Clearance) The apparent population mean clearance of tirzepatide is 0.061 L/h.[L41815] The mean steady-state apparent clearance of tirzepatide was 0.056 L/h.[A246260]

Absorpsi

Over the dose range of 1-5 mg, the C_max of tirzepatide ranged from 108 to 397 ng/mL.^A246260 The mean absolute bioavailability of tirzepatide following subcutaneous administration is 80%. Following subcutaneous administration, the T_max ranged from eight to 72 hours. The steady-state plasma concentrations were achieved following four weeks of once-weekly subcutaneous administration.^L41815 As tirzepatide delays gastric emptying, it has the potential to affect the absorption of concomitantly administered oral medications. The US prescribing information recommends the use of caution when co-administering tirzepatide with other oral medications.^L41815

Metabolisme

Tirzepatide is metabolized by proteolytic cleavage of the peptide backbone, beta-oxidation of the C20 fatty diacid moiety, and amide hydrolysis.^L41815

Rute Eliminasi

Tirzepatide is primarily excreted via urine and feces, mostly in the form of metabolites. Unchanged parent drug was not detectable in urine and feces.^L41815

Interaksi Makanan

1 Data

1. Take with or without food. Food has no clinically significant effects on drug exposure.

Interaksi Obat

614 Data

Pegvisomant	The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Tirzepatide.
Lipoic acid	The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Tirzepatide.
Moxifloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Moxifloxacin.
Grepafloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Grepafloxacin.
Enoxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Enoxacin.
Pefloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Pefloxacin.
Ciprofloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Ciprofloxacin.
Trovafloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Trovafloxacin.
Nalidixic acid	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Nalidixic acid.
Rosoxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Rosoxacin.
Cinoxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Cinoxacin.
Lomefloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Lomefloxacin.
Gatifloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Gatifloxacin.
Norfloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Norfloxacin.
Levofloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Levofloxacin.
Gemifloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Gemifloxacin.
Ofloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Ofloxacin.
Sparfloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Sparfloxacin.
Temafloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Temafloxacin.
Fleroxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Garenoxacin.
Nemonoxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Nemonoxacin.
Flumequine	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Flumequine.
Enrofloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Enrofloxacin.
Orbifloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Orbifloxacin.
Sarafloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Sarafloxacin.
Difloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Difloxacin.
Pazufloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Pazufloxacin.
Prulifloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Prulifloxacin.
Delafloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Delafloxacin.
Sitafloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Sitafloxacin.
Oxolinic acid	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Oxolinic acid.
Rufloxacin	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Rufloxacin.
Pipemidic acid	The therapeutic efficacy of Tirzepatide can be increased when used in combination with Pipemidic acid.
Methyclothiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Methyclothiazide.
Chlorthalidone	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Bendroflumethiazide.
Metolazone	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Metolazone.
Benzthiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Hydroflumethiazide.
Indapamide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Indapamide.
Chlorothiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Trichlormethiazide.
Polythiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Polythiazide.
Quinethazone	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Quinethazone.
Cyclopenthiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Cyclopenthiazide.
Epitizide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Epitizide.
Amitriptyline	Amitriptyline may decrease the hypoglycemic activities of Tirzepatide.
Protriptyline	Protriptyline may decrease the hypoglycemic activities of Tirzepatide.
Imipramine	Imipramine may decrease the hypoglycemic activities of Tirzepatide.
Nortriptyline	Nortriptyline may decrease the hypoglycemic activities of Tirzepatide.
Amoxapine	Amoxapine may decrease the hypoglycemic activities of Tirzepatide.
Trimipramine	Trimipramine may decrease the hypoglycemic activities of Tirzepatide.
Doxepin	Doxepin may decrease the hypoglycemic activities of Tirzepatide.
Desipramine	Desipramine may decrease the hypoglycemic activities of Tirzepatide.
Clomipramine	Clomipramine may decrease the hypoglycemic activities of Tirzepatide.
Amineptine	Amineptine may decrease the hypoglycemic activities of Tirzepatide.
Dimetacrine	Dimetacrine may decrease the hypoglycemic activities of Tirzepatide.
Butriptyline	Butriptyline may decrease the hypoglycemic activities of Tirzepatide.
Dosulepin	Dosulepin may decrease the hypoglycemic activities of Tirzepatide.
Tianeptine	Tianeptine may decrease the hypoglycemic activities of Tirzepatide.
Oxaprotiline	Oxaprotiline may decrease the hypoglycemic activities of Tirzepatide.
Opipramol	Opipramol may decrease the hypoglycemic activities of Tirzepatide.
Amitriptylinoxide	Amitriptylinoxide may decrease the hypoglycemic activities of Tirzepatide.
Dibenzepin	Dibenzepin may decrease the hypoglycemic activities of Tirzepatide.
Quinupramine	Quinupramine may decrease the hypoglycemic activities of Tirzepatide.
Melitracen	Melitracen may decrease the hypoglycemic activities of Tirzepatide.
Lofepramine	Lofepramine may decrease the hypoglycemic activities of Tirzepatide.
Iprindole	Iprindole may decrease the hypoglycemic activities of Tirzepatide.
Imipramine oxide	Imipramine oxide may decrease the hypoglycemic activities of Tirzepatide.
Dapagliflozin	Dapagliflozin may increase the hypoglycemic activities of Tirzepatide.
Canagliflozin	Canagliflozin may increase the hypoglycemic activities of Tirzepatide.
Leuprolide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Leuprolide.
Goserelin	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Goserelin.
Torasemide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Torasemide.
Nelfinavir	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Nelfinavir.
Indinavir	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Indinavir.
Ziprasidone	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Ziprasidone.
Etonogestrel	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Etonogestrel.
Desogestrel	Tirzepatide can cause a decrease in the absorption of Desogestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Olanzapine	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Olanzapine.
Megestrol acetate	Tirzepatide can cause a decrease in the absorption of Megestrol acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Clozapine	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Clozapine.
Levonorgestrel	Tirzepatide can cause a decrease in the absorption of Levonorgestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Progesterone	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Progesterone.
Chlorpromazine	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Chlorpromazine.
Haloperidol	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Haloperidol.
Ritonavir	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Ritonavir.
Piperazine	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Piperazine.
Medroxyprogesterone acetate	Tirzepatide can cause a decrease in the absorption of Medroxyprogesterone acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cyclothiazide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Cyclothiazide.
Niacin	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Niacin.
Epinephrine	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Epinephrine.
Furosemide	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Furosemide.
Norethisterone	Tirzepatide can cause a decrease in the absorption of Norethisterone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Risperidone	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Risperidone.
Pentamidine	The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Pentamidine.
Ethynodiol diacetate	Tirzepatide can cause a decrease in the absorption of Ethynodiol diacetate resulting in a reduced serum concentration and potentially a decrease in efficacy.

Target Protein

Glucagon-like peptide 1 receptor GLP1R

Gastric inhibitory polypeptide receptor GIPR

Referensi & Sumber

Artikel (PubMed)

PMID: 30473097
Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, Cui X, Briere DA, Cabrera O, Roell WC, Kuchibhotla U, Moyers JS, Benson CT, Gimeno RE, D'Alessio DA, Haupt A: 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. Mol Metab. 2018 Dec;18:3-14. doi: 10.1016/j.molmet.2018.09.009. Epub 2018 Oct 3.
PMID: 33030356
Frias JP: Tirzepatide: a glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) dual agonist in development for the treatment of type 2 diabetes. Expert Rev Endocrinol Metab. 2020 Nov;15(6):379-394. doi: 10.1080/17446651.2020.1830759. Epub 2020 Oct 8.
PMID: 33325008
Min T, Bain SC: The Role of Tirzepatide, Dual GIP and GLP-1 Receptor Agonist, in the Management of Type 2 Diabetes: The SURPASS Clinical Trials. Diabetes Ther. 2021 Jan;12(1):143-157. doi: 10.1007/s13300-020-00981-0. Epub 2020 Dec 15.

Link

Contoh Produk & Brand

Produk: 102 • International brands: 0

Produk

Mounjaro

Solution • 2.5 mg / 0.5 mL • Subcutaneous • Canada • Approved
Mounjaro

Solution • 5 mg / 0.5 mL • Subcutaneous • Canada • Approved
Mounjaro

Solution • 7.5 mg / 0.5 mL • Subcutaneous • Canada • Approved
Mounjaro

Solution • 10 mg / 0.5 mL • Subcutaneous • Canada • Approved
Mounjaro

Solution • 12.5 mg / 0.5 mL • Subcutaneous • Canada • Approved
Mounjaro

Solution • 15 mg / 0.5 mL • Subcutaneous • Canada • Approved
Mounjaro

Injection, solution • 2.5 mg/0.5mL • Subcutaneous • US • Approved
Mounjaro

Injection, solution • 5 mg/0.5mL • Subcutaneous • US • Approved

Menampilkan 8 dari 102 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.