Glucagon-Like Peptide-1 (GLP-1) Receptor Agonists - A Target Pipeline and Stakeholder Analysis 2012
This report “Glucagon-Like Peptide-1 (GLP-1) Receptor Agonists - A Target Pipeline and Stakeholder Analysis 2012” published in March 2012 provides a compilation of business, commercial, clinical and scientific information about GLP-1 receptor agonists. A comprehensive analysis of the state of the art and key trends guides the reader through this emerging antidiabetic drug class. Scientific and technological approaches as well as molecules in the target pipeline of GLP-1 receptor agonists are described and assessed. A critical appraisal of the clinical results of advanced GLP-1 receptor agonist projects and products is provided..
Scope of the report
Although the first glucagon-like peptide-1 receptor (GLP-1R) agonist was already approved in 2005, it was the launch of the once daily GLP-1R agonist Victoza from Novo Nordisk in 2010 which boosted the market size to US$ 1.7 bln in 2011. Victoza became a blockbuster in its second year on the market. The unique feature of weight reduction associated with the use GLP-1R agonists clearly differentiates this antidiabetic drug class from other established antidiabetics. The profound blood glucose lowering effect without significant hypoglycemia made GLP-1R agonists to a strongly emerging antidiabetic drug class. Gastrointestinal side effects such as nausea, vomiting and diarrhea seem to be associated with the pharmacologic effect of GLP-1R agonism.
The clinically and commercially validated target makes GLP-1 attractive for follow-on molecules with improved properties. Analysis of the GLP-1R agonist pipeline revealed in addition to the three approved and marketed GLP-1R agonists (Byetta, Victoza and once-weekly Bydureon) 66 R&D projects including eight life cycle versions. The vast majority of new GLP-1R agonists are designed to have improved features which mainly are based on convenience (less frequent administration or non-invasive/oral administration). Molecules with less frequent subcutaneous administration make out the majority (33) with 13 projects in clinical phases II or III, while 18 R&D projects are directed to non-invasive or oral administration of GLP-1R agonists with only one program in phase II. A strongly emerging third cluster of novel GLP-1 R agonists is that of GLP-1R agonists in combination with insulin at a fixed ratio and of co-agonists or dual targeting molecules, i.e. GLP-1R agonists which also act at the receptor of glucagon (mostly) or GIP.
Scope of the report
- Commercial experience with incretin-based therapeutics
- Monthly treatment costs of GLP-1R agonists
- Physician preferences and priorities for GLP-1R agonists
- GLP-1R agonist market drivers and restraints
- Unmet needs and differentiation between GLP-1R agonists
- Valuation of GLP-1R agonist programs by business transactions
- Next-to-market GLP-1R agonists
- Once-daily subcutaneous GLP-1R agonists
- Long-acting subcutaneous GLP-1R agonists
- Non-invasive peptide GLP-1R agonists
- Oral small molecule GLP-1R agonists
- Combinatgion and dual target Glucagon/GIP and GLP-1R agonists
Although the first glucagon-like peptide-1 receptor (GLP-1R) agonist was already approved in 2005, it was the launch of the once daily GLP-1R agonist Victoza from Novo Nordisk in 2010 which boosted the market size to US$ 1.7 bln in 2011. Victoza became a blockbuster in its second year on the market. The unique feature of weight reduction associated with the use GLP-1R agonists clearly differentiates this antidiabetic drug class from other established antidiabetics. The profound blood glucose lowering effect without significant hypoglycemia made GLP-1R agonists to a strongly emerging antidiabetic drug class. Gastrointestinal side effects such as nausea, vomiting and diarrhea seem to be associated with the pharmacologic effect of GLP-1R agonism.
The clinically and commercially validated target makes GLP-1 attractive for follow-on molecules with improved properties. Analysis of the GLP-1R agonist pipeline revealed in addition to the three approved and marketed GLP-1R agonists (Byetta, Victoza and once-weekly Bydureon) 66 R&D projects including eight life cycle versions. The vast majority of new GLP-1R agonists are designed to have improved features which mainly are based on convenience (less frequent administration or non-invasive/oral administration). Molecules with less frequent subcutaneous administration make out the majority (33) with 13 projects in clinical phases II or III, while 18 R&D projects are directed to non-invasive or oral administration of GLP-1R agonists with only one program in phase II. A strongly emerging third cluster of novel GLP-1 R agonists is that of GLP-1R agonists in combination with insulin at a fixed ratio and of co-agonists or dual targeting molecules, i.e. GLP-1R agonists which also act at the receptor of glucagon (mostly) or GIP.
1 OVERVIEW
2 EXECUTIVE SUMMARY
3 BACKGROUND OF INCRETIN-BASED THERAPY OF TYPE 2 DIABETES
4 COMMERCIAL EXPERIENCE WITH INCRETIN-BASED THERAPEUTICS
5 BUSINESS ENVIRONMENT FOR GLP-1R AGONISTS
5.1 Target validation and clinical proof-of-concept of GLP-1R agonists
5.2 Monthly treatment costs of GLP-1R agonists
5.3 Physician preferences and priorities for GLP-1R agonists
5.4 Diabetes patient population
5.5 GLP-1R agonist market drivers and restraints
5.6 Unmet needs and differentiation between GLP-1R agonists
5.7 Valuation of GLP-1R agonist programs by business transactions
6 GLP-1 RECEPTOR AGONIST PIPELINE
6.1 Overview of approaches in GLP-1R agonist pipeline
6.2 Next-to-market GLP-1R agonists
6.3 Once-daily subcutaneous GLP-1R agonists
6.4 Long-acting subcutaneous GLP-1R agonists
6.5 Non-invasive peptide GLP-1R agonists
6.6 Oral small molecule GLP-1R agonists
6.7 Insulin and GLP-1R agonists
6.8 Dual target Glucagon/GIP and GLP-1R agonists
6.9 Assessment of the GLP-1 receptor agonist pipeline
7 COMPANY PROFILES
Addex Pharmaceuticals
Alkermes
Altea Therapeutics
Alteogen
Amylin Pharmaceuticals
Arisaph Pharmaceuticals
Arisgen
Ascendis Pharma
Bio-ker (Multimedica)
Boehringer Ingelheim
BTG (Biocompatibles International)
Camurus
ConjuChem
Diartis Pharmaceuticals (Amunix)
Domain Therapeutics
Dong-A Pharmaceuticals
Eli Lilly
Emisphere Technologies
GlaxoSmithKline (Human Genome Science)
Hanmi Pharmaceutical
Intarcia Therapeutics
Johnson & Johnson (Centocor)
Lanthio Pharma
LG Life Sciences
MannKind
Merck & Co.
Novo Nordisk
Oramed Pharmaceuticals
Peptron & Neopharm
Pfizer
PharmaIn
PhaseBio
Poxel
PROLOR Biotech
Proxima Concepts (Diabetology)
Receptos
Roche
Sanofi-Aventis
Sanwa Kagaku Kenkyusho
Teijin
Transition Therapeutics
TransPharma Medical (assets acquired by Syneron)
Transtech Pharma
Uni-Bio Science
Zealand Pharma
Zydus Cadila
8 REFERENCES
9 TABLES
Table 1 Adverse effects and limitations of oral antidiabetics
Table 2 Byetta Sales 2005 – 2011
Table 3 GLP-1 Receptor Agonist Market
Table 4 DPP-IV Inhibitor Sales 2011
Table 5 Comparative Drug Profiles of Marketed GLP-1 Agonists
Table 6 Monthly treatment costs of GLP-1R Agonists
Table 7 Short- and Mid-Term GLP-1R Agonist Market Drivers and Restraints
Table 8 Differentiation factors for GLP-1R Agonists
Table 9 Overview of Approaches in Pipeline of GLP-1R Agonists
Table 10 Approaches followed by Big Pharma in R&D of GLP-1R agonists
Table 11 Potential Next-to-Market GLP-1R Agonists
Table 12 Daily Subcutaneous GLP-1 Receptor Agonists
Table 13 Technologies to increase the molecular size of GLP-1R agonists
Table 14 Weekly and Bi-weekly SC GLP-1 Receptor Agonists
Table 15 Comparative Drug Profiles of Advanced GLP-1 Agonists
Table 16 Monthly and Longer SC GLP-1 Receptor Agonists
Table 17 Non-Invasive Peptide GLP-1 Receptor Agonists
Table 18 Oral Small Molecule GLP-1 Receptor Agonists
Table 19 Fixed-Ratio Insulin and GLP-1 Receptor Agonist Combinations
Table 20 Dual Targeting GCG/GIP and GLP-1R Agonists
Table 21 Amylin pipeline of exenatide-based GLP-1R agonists
Table 22 GlaxoSmithKline’s pipeline of GLP-1R agonists
Table 23 Effects of ITCA 650 on HbA1c and body weight
Table 24 Novo Nordisk’s GLP-1 Receptor Agonist Pipeline
Table 25 Pfizer’s pipeline of GLP-1 receptor agonists
Table 26 Overview of taspoglutide side effects at 24 weeks:
Table 27 Sanofi’s GLP-1 Receptor Agonist Pipeline
Table 28 Sanofi’s phase III program of lixisenatide
ADDENDUM
A Executive Drug Profiles
Albiglutide (GSK716155)
Bydureon
CJC-1134-PC
CM3
CNTO3649 / CNTO736
DA-3091
Dulaglutide (LY2189265)
Liraglutide
Lixisenatide
PF-04856883
B Competitor Analysis
GLP-1 Receptor Agonists in Metabolic Diseases
GLP-1 Receptor Agonists in Other Diseases
Discontinued GLP-1 Receptor Agonist Projects
2 EXECUTIVE SUMMARY
3 BACKGROUND OF INCRETIN-BASED THERAPY OF TYPE 2 DIABETES
4 COMMERCIAL EXPERIENCE WITH INCRETIN-BASED THERAPEUTICS
5 BUSINESS ENVIRONMENT FOR GLP-1R AGONISTS
5.1 Target validation and clinical proof-of-concept of GLP-1R agonists
5.2 Monthly treatment costs of GLP-1R agonists
5.3 Physician preferences and priorities for GLP-1R agonists
5.4 Diabetes patient population
5.5 GLP-1R agonist market drivers and restraints
5.6 Unmet needs and differentiation between GLP-1R agonists
5.7 Valuation of GLP-1R agonist programs by business transactions
6 GLP-1 RECEPTOR AGONIST PIPELINE
6.1 Overview of approaches in GLP-1R agonist pipeline
6.2 Next-to-market GLP-1R agonists
6.3 Once-daily subcutaneous GLP-1R agonists
6.4 Long-acting subcutaneous GLP-1R agonists
6.5 Non-invasive peptide GLP-1R agonists
6.6 Oral small molecule GLP-1R agonists
6.7 Insulin and GLP-1R agonists
6.8 Dual target Glucagon/GIP and GLP-1R agonists
6.9 Assessment of the GLP-1 receptor agonist pipeline
7 COMPANY PROFILES
Addex Pharmaceuticals
Alkermes
Altea Therapeutics
Alteogen
Amylin Pharmaceuticals
Arisaph Pharmaceuticals
Arisgen
Ascendis Pharma
Bio-ker (Multimedica)
Boehringer Ingelheim
BTG (Biocompatibles International)
Camurus
ConjuChem
Diartis Pharmaceuticals (Amunix)
Domain Therapeutics
Dong-A Pharmaceuticals
Eli Lilly
Emisphere Technologies
GlaxoSmithKline (Human Genome Science)
Hanmi Pharmaceutical
Intarcia Therapeutics
Johnson & Johnson (Centocor)
Lanthio Pharma
LG Life Sciences
MannKind
Merck & Co.
Novo Nordisk
Oramed Pharmaceuticals
Peptron & Neopharm
Pfizer
PharmaIn
PhaseBio
Poxel
PROLOR Biotech
Proxima Concepts (Diabetology)
Receptos
Roche
Sanofi-Aventis
Sanwa Kagaku Kenkyusho
Teijin
Transition Therapeutics
TransPharma Medical (assets acquired by Syneron)
Transtech Pharma
Uni-Bio Science
Zealand Pharma
Zydus Cadila
8 REFERENCES
9 TABLES
Table 1 Adverse effects and limitations of oral antidiabetics
Table 2 Byetta Sales 2005 – 2011
Table 3 GLP-1 Receptor Agonist Market
Table 4 DPP-IV Inhibitor Sales 2011
Table 5 Comparative Drug Profiles of Marketed GLP-1 Agonists
Table 6 Monthly treatment costs of GLP-1R Agonists
Table 7 Short- and Mid-Term GLP-1R Agonist Market Drivers and Restraints
Table 8 Differentiation factors for GLP-1R Agonists
Table 9 Overview of Approaches in Pipeline of GLP-1R Agonists
Table 10 Approaches followed by Big Pharma in R&D of GLP-1R agonists
Table 11 Potential Next-to-Market GLP-1R Agonists
Table 12 Daily Subcutaneous GLP-1 Receptor Agonists
Table 13 Technologies to increase the molecular size of GLP-1R agonists
Table 14 Weekly and Bi-weekly SC GLP-1 Receptor Agonists
Table 15 Comparative Drug Profiles of Advanced GLP-1 Agonists
Table 16 Monthly and Longer SC GLP-1 Receptor Agonists
Table 17 Non-Invasive Peptide GLP-1 Receptor Agonists
Table 18 Oral Small Molecule GLP-1 Receptor Agonists
Table 19 Fixed-Ratio Insulin and GLP-1 Receptor Agonist Combinations
Table 20 Dual Targeting GCG/GIP and GLP-1R Agonists
Table 21 Amylin pipeline of exenatide-based GLP-1R agonists
Table 22 GlaxoSmithKline’s pipeline of GLP-1R agonists
Table 23 Effects of ITCA 650 on HbA1c and body weight
Table 24 Novo Nordisk’s GLP-1 Receptor Agonist Pipeline
Table 25 Pfizer’s pipeline of GLP-1 receptor agonists
Table 26 Overview of taspoglutide side effects at 24 weeks:
Table 27 Sanofi’s GLP-1 Receptor Agonist Pipeline
Table 28 Sanofi’s phase III program of lixisenatide
ADDENDUM
A Executive Drug Profiles
Albiglutide (GSK716155)
Bydureon
CJC-1134-PC
CM3
CNTO3649 / CNTO736
DA-3091
Dulaglutide (LY2189265)
Liraglutide
Lixisenatide
PF-04856883
B Competitor Analysis
GLP-1 Receptor Agonists in Metabolic Diseases
GLP-1 Receptor Agonists in Other Diseases
Discontinued GLP-1 Receptor Agonist Projects
