On May 21st, the Chinese National Medical Products Administration (NMPA) approved Tirzepatide (brand name Mounjaro), a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist developed by Lilly, for the improvement of glycemic control in adults with type 2 diabetes. 

src: NMPA

Tirzepatide is a once-weekly injectable GIP and GLP-1 receptor agonist. GLP-1 and GIP are two naturally occurring incretins that regulate glucose and energy homeostasis. Studies suggest that when combined with a GLP-1 receptor agonist, GIP may lead to greater impacts on glycemic control and weight loss. 

Trials

For type 2 diabetes, Lilly initiated the large SURPASS clinical trial program consisting of 10 studies, including head-to-head comparisons of Mounjaro (5mg, 10mg, and 15mg) with semaglutide 1mg, insulin glargine, and insulin degludec. Across the SURPASS program, Mounjaro 5mg led to a mean HbA1c reduction of 1.8-2.1%, while the 10mg and 15mg doses reduced HbA1c by 1.7-2.4% on average. 

The approval in China was mainly based on the positive results from the SURPASS program and the SURPASS-AP-Combo phase 3 trial, which enrolled type 2 diabetes patients inadequately controlled on metformin alone. 98.3% participants were Asian (n=917), and 83.4% were Chinese (n=763). After 40 weeks, Mounjaro (5mg, 10mg, and 15mg) demonstrated non-inferiority to titrated insulin glargine in HbA1c reduction and weight loss. 

Moreover, Tirzepatide achieved significant weight loss across four phase 3 studies (SURMOUNT-1, -2, -3, and -4) in individuals with and without diabetes. In SURMOUNT-1 with non-diabetic obese participants (mean weight 104.8kg, mean BMI 38kg/m2), once-weekly subcutaneous Tirzepatide 15mg led to ~8% weight loss at week 12 and up to ~16% at week 36. At week 72, mean weight loss was 22.5% (24kg) with Tirzepatide 5mg, 10mg, and 15mg. 

In SURMOUNT-2 with type 2 diabetes and obesity, Tirzepatide 10mg and 15mg led to 15.7% (15.6kg) and 13.4% (13.5kg) weight loss respectively at week 72, with 81.6% and 86.4% achieving ≥5% weight loss (vs 30.5% with placebo). Both SURMOUNT-3 (obesity without diabetes) and SURMOUNT-4 (weight loss maintenance) also met primary and key secondary endpoints. 

Tirzepatide at FDA

Index	Route	Brand Name	Labeler	Approval Date	Dosage
1	SOLUTION;SUBCUTANEOUS	ZEPBOUND	ELI LILLY AND CO	Mar 28, 2024	10MG/0.5ML (10MG/0.5ML)
2	SOLUTION;SUBCUTANEOUS	ZEPBOUND (AUTOINJECTOR)	ELI LILLY AND CO	Nov 8, 2023	10MG/0.5ML (10MG/0.5ML)
3	SOLUTION;SUBCUTANEOUS	MOUNJARO (AUTOINJECTOR)	ELI LILLY AND CO	May 13, 2022	10MG/0.5ML (10MG/0.5ML)
4	SOLUTION;SUBCUTANEOUS	ZEPBOUND (AUTOINJECTOR)	ELI LILLY AND CO	Nov 8, 2023	2.5MG/0.5ML (2.5MG/0.5ML)
5	SOLUTION;SUBCUTANEOUS	ZEPBOUND (AUTOINJECTOR)	ELI LILLY AND CO	Nov 8, 2023	15MG/0.5ML (15MG/0.5ML)
6	SOLUTION;SUBCUTANEOUS	ZEPBOUND	ELI LILLY AND CO	Mar 28, 2024	15MG/0.5ML (15MG/0.5ML)
7	SOLUTION;SUBCUTANEOUS	MOUNJARO (AUTOINJECTOR)	ELI LILLY AND CO	May 13, 2022	5MG/0.5ML (5MG/0.5ML)
8	SOLUTION;SUBCUTANEOUS	MOUNJARO (AUTOINJECTOR)	ELI LILLY AND CO	May 13, 2022	2.5MG/0.5ML (2.5MG/0.5ML)
9	SOLUTION;SUBCUTANEOUS	ZEPBOUND (AUTOINJECTOR)	ELI LILLY AND CO	Nov 8, 2023	5MG/0.5ML (5MG/0.5ML)
10	SOLUTION;SUBCUTANEOUS	MOUNJARO (AUTOINJECTOR)	ELI LILLY AND CO	May 13, 2022	12.5MG/0.5ML (12.5MG/0.5ML)
11	SOLUTION;SUBCUTANEOUS	ZEPBOUND	ELI LILLY AND CO	Mar 28, 2024	5MG/0.5ML (5MG/0.5ML)
12	SOLUTION;SUBCUTANEOUS	MOUNJARO (AUTOINJECTOR)	ELI LILLY AND CO	May 13, 2022	15MG/0.5ML (15MG/0.5ML)
13	SOLUTION;SUBCUTANEOUS	ZEPBOUND	ELI LILLY AND CO	Mar 28, 2024	2.5MG/0.5ML (2.5MG/0.5ML)
14	SOLUTION;SUBCUTANEOUS	MOUNJARO	ELI LILLY AND CO	Jul 28, 2023	12.5MG/0.5ML (12.5MG/0.5ML)
15	SOLUTION;SUBCUTANEOUS	ZEPBOUND (AUTOINJECTOR)	ELI LILLY AND CO	Nov 8, 2023	7.5MG/0.5ML (7.5MG/0.5ML)
16	SOLUTION;SUBCUTANEOUS	MOUNJARO	ELI LILLY AND CO	Jul 28, 2023	15MG/0.5ML (15MG/0.5ML)
17	SOLUTION;SUBCUTANEOUS	MOUNJARO	ELI LILLY AND CO	Jul 28, 2023	5MG/0.5ML (5MG/0.5ML)
18	SOLUTION;SUBCUTANEOUS	MOUNJARO	ELI LILLY AND CO	Jul 28, 2023	7.5MG/0.5ML (7.5MG/0.5ML)
19	SOLUTION;SUBCUTANEOUS	MOUNJARO (AUTOINJECTOR)	ELI LILLY AND CO	May 13, 2022	7.5MG/0.5ML (7.5MG/0.5ML)
20	SOLUTION;SUBCUTANEOUS	MOUNJARO	ELI LILLY AND CO	Jul 28, 2023	10MG/0.5ML (10MG/0.5ML)
21	SOLUTION;SUBCUTANEOUS	ZEPBOUND	ELI LILLY AND CO	Mar 28, 2024	12.5MG/0.5ML (12.5MG/0.5ML)
22	SOLUTION;SUBCUTANEOUS	ZEPBOUND (AUTOINJECTOR)	ELI LILLY AND CO	Nov 8, 2023	12.5MG/0.5ML (12.5MG/0.5ML)
23	SOLUTION;SUBCUTANEOUS	MOUNJARO	ELI LILLY AND CO	Jul 28, 2023	2.5MG/0.5ML (2.5MG/0.5ML)
24	SOLUTION;SUBCUTANEOUS	ZEPBOUND	ELI LILLY AND CO	Mar 28, 2024	7.5MG/0.5ML (7.5MG/0.5ML)

In November 2023, the FDA approved Tirzepatide (brand Zepbound) for chronic weight management in adults with obesity (BMI ≥30kg/m2) or overweight (BMI ≥27kg/m2) with at least one weight-related comorbidity. The weight management indication in China is currently under review by the NMPA. Tirzepatide is currently protected by three patents.

Patent Number	Submission Date	Expiration Date	Drug Substance Patent?	Drug Product Patent?
9474780	Jun 9, 2022	Jan 5, 2036	Y	Y
11357820	Jun 30, 2022	Jun 14, 2039		Y
11918623	Mar 28, 2024	Jun 14, 2039

References

PHARMCUBE article