💉 GLP-1 Receptor Agonist Drug Profiles
GLP-1 receptor agonists (GLP-1 RAs) represent the absolute core of the contemporary peptide drug landscape. This chapter provides comprehensive profiles of the five major marketed GLP-1 drugs, covering structure, clinical data, market performance, and competitive dynamics.
1. Semaglutide
| Attribute |
Details |
| Structural Class |
31-amino acid GLP-1 analog, C18 fatty acid side chain (Aib8, Arg34) |
| CAS Number |
910463-68-2 |
| Molecular Formula |
C₁₈₇H₂₉₁N₄₅O₅₉ |
| Molecular Weight |
4113.58 g/mol |
| Brand Names |
Ozempic (injectable glucose control 0.5/1.0 mg), Wegovy (injectable weight loss 2.4 mg), Rybelsus (oral 3/7/14 mg) |
| Originator |
Novo Nordisk |
| Mechanism of Action |
GLP-1 receptor agonist → promotes insulin secretion → suppresses glucagon → delays gastric emptying → reduces appetite |
Indications & Approval Status
| Indication |
Approved Regions |
Approval Year |
Notes |
| Type 2 Diabetes (Ozempic) |
US, EU, China |
2017–2021 |
First once-weekly GLP-1 RA globally |
| Obesity/Overweight (Wegovy) |
US, EU, China |
2021–2024 |
Launched in China 2023 |
| Type 2 Diabetes (Rybelsus oral) |
US, EU, China |
2019–2024 |
First oral GLP-1 drug |
| Cardiovascular Benefit (CVD) |
US, EU |
2024 |
SELECT study confirmed 20% MACE risk reduction |
| Heart Failure (HFpEF) |
US |
2025 |
STEP-HFpEF positive results |
| MASH (Metabolic Steatohepatitis) |
Phase III |
— |
ESSENCE study ongoing |
| CKD (Chronic Kidney Disease) |
Phase III |
— |
FLOW study terminated early (positive) |
Sales Data
| Year |
Ozempic ($B) |
Wegovy ($B) |
Rybelsus ($B) |
Total ($B) |
YoY Growth |
| 2020 |
5.2 |
— |
0.3 |
5.5 |
— |
| 2021 |
7.6 |
0.8 |
0.6 |
9.0 |
+64% |
| 2022 |
10.9 |
2.3 |
1.2 |
14.4 |
+60% |
| 2023 |
14.2 |
4.5 |
1.9 |
20.6 |
+43% |
| 2024 |
16.8 |
6.8 |
2.8 |
26.4 |
+28% |
Patent & Generic Competition
| Region |
Core Patent Expiry |
Generics / Biosimilars Activity |
| China |
2026 (compound patent) |
Nuotai Bio, Shengnuo Bio, Hybio Pharmaceutical have filed registration applications |
| US |
2031–2032 (US patent extension) |
Multiple generics in ANDA stage |
| EU |
2026–2030 (staggered patent expiry) |
Generics began filing EMA applications from 2025 |
2. Tirzepatide
| Attribute |
Details |
| Structural Class |
39-amino acid GIP/GLP-1 dual receptor agonist (GIPR/GLP-1R dual activation) |
| CAS Number |
2023788-19-2 |
| Molecular Weight |
4814.52 g/mol |
| Brand Names |
Mounjaro (glucose control), Zepbound (weight loss) |
| Originator |
Eli Lilly |
| Mechanism of Action |
Simultaneously activates GIP and GLP-1 receptors → synergistic insulin secretion → stronger appetite suppression → significant weight loss |
Indications & Approval Status
| Indication |
Approved Regions |
Approval Year |
Notes |
| Type 2 Diabetes |
US, EU, China |
2022–2024 |
SURPASS trial series |
| Obesity/Overweight |
US, EU, China |
2023–2024 |
SURMOUNT trial series |
| MASH |
Phase III |
— |
SYNERGY-NASH study |
| Heart Failure |
Phase III |
— |
SUMMIT study |
| Sleep Apnea |
2024 Approved |
— |
SURMOUNT-OSA study |
Sales Data
| Year |
Mounjaro/Zepbound ($B) |
YoY Growth |
| 2022 |
0.5 |
— |
| 2023 |
5.2 |
+940% |
| 2024 |
11.5 |
+121% |
Patent & Competition
| Region |
Core Patent Expiry |
Competitive Dynamics |
| Global |
~2036–2039 |
Long patent life; Chinese dual-target GLP-1 drugs (HRS9531, etc.) actively catching up |
3. Liraglutide
| Attribute |
Details |
| Structural Class |
31-amino acid GLP-1 analog, C16 fatty acid side chain |
| CAS Number |
204656-20-2 |
| Brand Names |
Victoza (glucose control), Saxenda (weight loss) |
| Originator |
Novo Nordisk |
| Year |
Victoza + Saxenda ($B) |
| 2020 |
3.6 |
| 2022 |
2.8 |
| 2024 |
1.8 (declining due to semaglutide substitution effect) |
4. Dulaglutide
| Attribute |
Details |
| Structural Class |
GLP-1 analog-Fc fusion protein (not a pure peptide) |
| CAS Number |
923950-08-7 |
| Brand Name |
Trulicity |
| Originator |
Eli Lilly |
| Year |
Trulicity ($B) |
| 2022 |
7.4 |
| 2024 |
5.5 (declining due to tirzepatide substitution effect) |
5. Exenatide
| Attribute |
Details |
| Structural Class |
39 amino acids, synthetic version of natural Exendin-4 |
| CAS Number |
141758-74-9 |
| Brand Names |
Byetta (twice daily), Bydureon (once weekly) |
| Originator |
AstraZeneca (originally Amylin/BMS) |
| Year |
Byetta + Bydureon ($B) |
| 2020 |
0.5 |
| 2024 |
<0.2 |
6. GLP-1 Drug Comparative Analysis
| Drug |
Molecular Size |
Half-Life |
Dosing Frequency |
HbA1c Reduction |
Weight Loss |
2024 Sales ($B) |
| Semaglutide |
31aa |
7 days |
QW / PO QD |
1.5–2.0% |
12–15% |
26.4 |
| Tirzepatide |
39aa |
5 days |
QW |
2.0–2.5% |
15–22% |
11.5 |
| Liraglutide |
31aa |
13h |
QD |
1.0–1.5% |
5–8% |
1.8 |
| Dulaglutide |
Fc fusion |
5 days |
QW |
1.2–1.8% |
3–5% |
5.5 |
| Exenatide |
39aa |
2.4h |
BID / QW |
0.8–1.5% |
3–5% |
<0.2 |
7. Biosimilars & Next-Generation GLP-1 Pipeline
| Candidate |
Company |
Target |
Phase |
Differentiation |
| Retatrutide |
Eli Lilly |
GLP-1/GIP/Glucagon |
Ph3 |
Triple agonist, up to 24% weight loss |
| Orforglipron |
Eli Lilly |
GLP-1 RA (oral non-peptide small molecule) |
Ph3 |
Oral small molecule, once daily |
| Survodutide |
Boehringer/Zydus |
GLP-1/Glucagon |
Ph3 |
Leading in MASH indication |
| Mazdutide |
Innovent Biologics |
GLP-1/Glucagon |
Ph3 (China) |
Fastest dual-target in China |
| Ecnoglutide |
Sciwind Biosciences |
GLP-1 RA (long-acting) |
Ph3 |
Phase 3 data showing excellent efficacy |
Data Sources: Novo Nordisk/Eli Lilly/AstraZeneca annual reports, FDA/EMA/NMPA approval information, ClinicalTrials.gov, EvaluatePharma. For GLP-1 API supply chain mapping, CDMO capacity allocation, or generic drug registration progress updates, visit SENO Biotechnology for specialized GLP-1 deep-dive reports and customized market intelligence.