Tirzepatide
- CAS No.
- 2023788-19-2
- Chemical Name:
- Tirzepatide
- Synonyms
- GLP-1 RA;Tilpotide;Tilposide;GIP\GLP-1;Tirzepatide;Trizepatide;terzapitide;tirzepatide 10mg;Tirzepatide(GLP-1);Trizepatide peptide
- CBNumber:
- CB24869395
- Molecular Formula:
- Molecular Weight:
- 0
- MOL File:
- Mol file
- Modify Date:
- 2024/8/8 18:06:34
| storage temp. | Store at -20°C |
|---|---|
| solubility | Soluble in DMSO |
| form | Solid |
| color | White to off-white |
| Sequence | Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{diacid-C20-gamma-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 |
Tirzepatide Chemical Properties,Uses,Production
Description
Tirzepatide (LY3298176) was developed as a dual agonist to both GLP-1 and gastric inhibitory polypeptide (GIP) receptors (Frias et al., 2018). Similar to GLP-1, GIP is an incretin hormone that functions to induce insulin secretion.
Uses
Tirzepatide is used with a proper diet and exercise program to control high blood sugar in people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems.
Definition
Mounjaro® and Ozempic® have distinct active ingredients: tirzepatide and semaglutide, respectively. However, both of these drugs are GLP-1 agonists, which bind to GLP-1 receptors, simulate a feeling of satiety, and signal the pancreas to produce insulin.
Trade name
brand name: Mounjaro
Mechanism of action
It works to stimulate first- and second-phase insulin secretion, and reduces glucagon levels, both in a glucose-dependent manner. Tirzepatide was also shown to delay gastric emptying, lower fasting and postprandial glucose concentration, decrease food intake, 4 and reduce body weight in patients with type 2 diabetes.
Side effects
The overall safety and tolerability profile of tirzepatide was similar to other incretin-based therapies that have been approved for the treatment of obesity. This said, reported side effects were considerable, especially as dosage levels increased. The most common adverse events were nausea (~30%), diarrhea (~20%), constipation (~15%) and vomiting (~10%).
If tirzepatide gets approved as a both a blood glucose control and anti-obesity agent, it could become a blockbuster drug. However, this isn’t a sure thing. It will have to overcome pricing and reimbursement obstacles, which have plagued similar treatments.
Synthesis
The synthesis process of tirzepatide is as follows: to a reactor was charged dichloromethane (28.6 kg), water (5.4 kg), DTT (4.3 kg), Boc-Fragment 1 + 2 + 3 + 4 (14.3 kg, 8), and TIPS (3.3 kg), resulting in a slurry. The slurry was cooled to less than 10 °C before TFA (162 kg) was added over no more than 1.75 h, resulting in a solution. The solution was warmed to 21 °C and held at this temperature for 3 h. The solution was transferred to a separate reactor, rinsing with TFA (54.3 kg). This solution was cooled to ?10 °C and charged MTBE (125.8 kg) over 2 h. Then, additional MTBE (233 kg) was charged at 17 kg/h, maintaining an internal temperature of less than ?5 °C. The resulting slurry was warmed to 0 °C and then filtered. The wet cake was washed with MTBE (2 × 11 kg/kg relative to 8) and then dried under vacuum at no more than 35 °C to obtain tirzepatide (1, 8.71 kg, 1.81 mol, 81% yield)[1].
Clinical claims and research
Tirzepatide (Eli Lilly), a novel, once-weekly injectable dual glucose-dependent insulinotropic polypeptide (GIP) receptor and GLP-1 RA combination drug, has been developed to treat patients with T2DM. The manufacturer (Eli Lilly) announced the submission of a biologics license application with priority review to the FDA for T2DM on October 27, 2021, with a decision expected in mid-2022.
Research
Tirzepatide is in phase 3 clinical development at Eli Lilly and Company for blood glucose management in adults with type 2 diabetes, chronic weight management, and obesity-related heart failure with preserved ejection fraction. In addition, Tirzepatide is being studied as a potential treatment for non-alcoholic steatohepatitis (NASH). The molecule comprises a 39 amino acid peptide backbone and a side chain at residue 20. Of the 39 amino acids, 37 are naturally occurring (or coded), while two are noncoded aminoisobutyric acid residues at positions 2 and 13[1].
References
[1] Calley, J. and W. Dhillo. “Effects of the Hormone Kisspeptin on Reproductive Hormone Release in Humans.” 2014. 0.
Tirzepatide Preparation Products And Raw materials
Raw materials
Preparation Products
Tirzepatide Suppliers
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
| Apicore Pharmaceuticals Pvt Ltd | +91-2662267177 +91-2662267166 | Gujarat, India | 181 | 58 | Inquiry |
| Shanghai Longyu Biotechnology Co., Ltd. | +8613917842738 | China | 2534 | 58 | Inquiry |
| Hubei Yuanao Technology CO Ltd | +86-15377628618 +86-15377628618 | China | 6 | 58 | Inquiry |
| HangZhou RunYan Pharma Technology Co.,LTD. | +86-88660901 +86-18112526015 | China | 326 | 58 | Inquiry |
| Shanghai Getian Industrial Co., LTD | +86-15373193816 +86-15373193816 | China | 269 | 58 | Inquiry |
| Hebei Lingding Biotechnology Co., Ltd. | +86-18031140164 +86-19933155420 | China | 198 | 58 | Inquiry |
| Hebei Mojin Biotechnology Co., Ltd | +8613288715578 | China | 12455 | 58 | Inquiry |
| Wuhan Cell Pharmaceutical Co., Ltd | +86-13129979210 +86-13129979210 | China | 376 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
Related articles
- Is tirzepatide available for weight loss?
- Tirzepatide works for weight loss by decreasing your appetite and slowing the movement of food from the stomach into the small....
- Mar 20，2024