Oral Diabetes Drugs

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Diabetes is a disease caused by high levels of blood glucose resulting from improper production of insulin or action of insulin.

  • Type 1: In this Diabetes, the cells that make the hormone insulin regulate the blood glucose are destroyed by the body immune system. This is also called as juvenile onset diabetes as it occurs mainly in children and young adults. 5%-10% of all the cases of diabetes have Type I diabetes. Clinical trials are being pursued and planned to prevent type I diabetes. This is also called as Insulin Dependent Diabetes Mellitus (IDDM).
  • Type 2: In this case, either the cells do not use insulin properly or the body does not produce enough insulin. 90% - 95% of the diabetics have Type 2 diabetes. This type of disease is also called as non-insulin dependent diabetes mellitus (NIDDM) and is mainly observed in people with old age, obese, family history of diabetes, history of gestational diabetes, impaired glucose metabolism, physical inactivity and race/ethnicity.
  • Gestational Diabetes: Increase in the levels of blood sugar during pregnancy is called gestational diabetes.

Incidence and prevalence


In year 2004, diabetes ( Both type I and type II ) was diagnosed in 1.4 million adults between the age of 18-79 years (Figure 1). The incidence of diabetes was lower in adults having an age between 18-44 years compared to other groups (Figure 2). From 1997 through 2004, the age adjusted incidence of diagnosed diabetes ( Both type I and type II )increased by 35% among men and 46% among women (Figure 3).

Figure 1. Annual number (in thousands) of new cases of diagnosed diabetes among adults aged 18-79 years, in United States from 1997-2004. Source
Figure 3. Gender based incidence of diagnosed diabetes per 1000 population aged from 18-79 years in U.S. Source
Figure 2. Incidence of diagnosed diabetes per 1000 population aged 18-79 years, by age in U.S from 1997 to 2004. Source
S.NO Country/Region Extrapolated incidence
1 USA 861,533
2 Canada 95,372
3 Europe 1,474,002
4 Asia 10,063,645
5 Africa 1,290,255
6 Middle east 1,055,809
7 Australia and Southern Pacific 70,138

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The prevalence of diabetes( Both type I and type II ) in U.S. during the years 1980 to 2005, increased from 5.6 million to 15.8 million (Figure 4). Especially people aged from 65 to 74 had the highest prevalence compared to other age groups (Figure 5). The prevalence of the disease was similar in both men and women till the year 1998 but from 1999, the prevalence of the disease increased highly in men compared to females (Figure 6).

Figure 4. Number (millions) of persons with diagnosed diabetes from year 1980 to 2005 in United States. Source
Figure 5. Age dependent Prevalence of diagnosed diabetes in United States from year 1980 to 2005. Source
Figure 6. Gender dependent Prevalence of diagnosed diabetes in United States from year 1980 to 2005. Source
S.NO Country/Region Extrapolated Prevalence
1 USA 17,273,847
2 Canada 1,912,227
3 Europe 33,882,009
4 Asia 201,777,550
5 Africa 25,393,535
6 Middle east 21,169,243
7 Australia and Southern Pacific 1,406,291

Market Overview

  • The Insulin market in 2006 was largely dominated by two players, Novo Nordisk of Denmark and Eli Lilly of USA.
  • India and China are emerging as the most potential future markets for insulin delivery devices.
  • Growing at a CAGR of 14.09%, global insulin market will reach US$ 14.5 Billion by 2010 from US$ 7.5 Billion in 2005.
  • Over 60% of the insulin sold in 2006 was sold in pen devices.
  • Insulin pen devices dominate the market in Europe and Japan whereas syringes and pumps dominate the US market.
  • There was a big improvement in the global diabetes market for innovation particularly in the field of non-invasive methods of insulin delivery, including inhalable, oral and patch technology. Source
  • There are 3 key new OAD classes; PPAR agonists, GLP-1 agonists/DPP IV inhibitors, and amlinomimetic agents. High forecasted sales are anticipated in 2011 for the GLP-1 agonist Exenatide LAR and the DPP-IV inhibitor Galvus at $2,902.9m and $1,228.7m, respectively. Source
Diabetic market data.jpeg

A. Competitive dynamics of the leading players in the global diabetes market, 2005 B. Global diabetes market share by geography, 2005] C. Worldwide Diabetes Market, 2000, 2001, 2002 and 2007 D. Global* market share of leading insulins (%), 1999-2003

Product Information

Overall categorization of diabetes treatments

Products: Oral Hypoglycemic Agents

Oral Hypoglycemic Agents
Drug Brand Company Availability
First Generation      
Acetohexomide Dymelor Eli Lilly US, F, G, I, S,UK, J
Chlorpropamide, Tolazamide Diabenase Pfizer US, F, G, I, S,UK, J
Second Generation      
Glyburide (Glibenclamide) Diabeta Aventis US, F, G, I, S,UK, J
Glyburide (Glibenclamide) Micronase Pharmacia US, F, G, I, S,UK, J
Glyburide (Glibenclamide) Glynase Pharmacia US, F, G, I, S,UK, J
Glypizide Glucotrol, Glucotrol XL Pfizer US, F, G, I, S,UK, J
Third Generation      
Glimepride Amaryl Aventis US, F, G, I, S,UK, J
Repaglinide Prandin Novo Nordisk US, F, G, I, S,UK, J
Nateglinide Sralix Novartis US,UK, J
Metfromin Glucophage, Glucophage XR Bristol-Myers Squibb US
Rosiglitazone Avandia Glaxosmithkline US, G, UK
Pioglitazone Actos Takeda/ Eli Lilly US, UK, G, S, J
Alfa-Glucosidase Inhibitors
Acarbose Precose Bayer US, F, G, I, S,UK, J
Miglitol Glyset Pharmacia US, F, G, S
Voglibose Basen, Volix, Vogseal Ranbaxy, Nihon Pharmaceutical Industry Ltd I, J
Dipeptidyl peptidase-4 (DPP-4) inhibitor
Sitgliptin Januvia Merck US

Products: Fixed Drug Combinations

Fixed Drug Combinations
Brand Name Drug 1 Drug 2 Company
Metaglip Glipizide Metformin Bristol-Myers Squibb
Duetact Glimepiride Pioglitazone Takeda
Avandaryl Glimepiride Rosiglitazone GlaxoSmithKline
ACTOSPlusMet Pioglitazone Metformin Takeda
Avandamet Rosiglitazone Metformin GlaxoSmithKline
Janumet Sitgliptin Metformin Merck

Product pipeline

Product Pipeline
Drug Company Stage
Dipeptidyl Peptidase IV (DPP-IV) Inhibitor :DPP-IV inactivates glucagon-like peptide-1 (GLP-1), an important mediator of blood glucose levels following meals. DPP-IV inhibitors have been clinically shown to provide long term improvement of glucose control without the risk of hypoglycemia, and to improve the function of pancreatic beta cells, the cells responsible for the production of insulin.
ALS 2-0426 Alantos Pharmaceuticals, Amgen, Servier 1
PSN9301 OSI 2
SYR-322 Takeda 3
R1579 Roche 1
vildagliptin (Galvus) novartis NDA submitted in March 2006
MP-513 Mitsubishi Pharma 2
Gastrin + DPP IV Inhibitor Transition Therapeutics Preclinical
Saxagliptin Otsuka Pharmaceutical Co, Bristol-Myers Squibb 3
Insulin sensitizer
ISIS 113715 Isis 3
NCX 4016 (Nitric Oxide donating derivative of Acetyl Salicylic acid) NicOx 2
DG070 inhibitors Develogen AG Preclinical
NovoNorm® (repaglinide)/Metformin Novo Nordisk 3
Gastrin + Metformin Transition Therapeutics 1
GLP 1 Analogue / Agonists GLP 1 Analogues have to be injected subcutaneously, Emisphere is working on an oral analogue
Abiglutide (716155) glaxosmithkline 2
TH0318 Theratechnolgies 1
Liraglutide (NN2211) Novo Nordisk 3
R1583 Roche 2
Oral GLP Emisphere Technologies 1
PC-DAC™:Exendin-4 ConjuChem 2
  Bristol-Myers Squibb Exploratory development
AVE0001A Sanofi Aventis 2
Gastrin +GLP 1 Agonist Transition Therapeutics 2
Peroxisome Proliferator-Activated Receptor (PPAR) agonist/analogue
CS-011 (Rivoglitazone) Sankyo 2
Metaglidasen(MBX 102) Metabolex 2
MBX-2044 Metabolex 1
AVE8134 Sanofi Aventis 2
AVE0897 Sanofi Aventis 1
R1439, aleglitazar Roche 2
AVE0847 Sanofi Aventis 2
SAR351034 Sanofi Aventis Preclinical
376501 Glaxosmithkline 1
625019 Glaxosmithkline 1
677954 Glaxosmithkline 2
Avandia Glaxosmithkline 2
Avandia XR Glaxosmithkline 2
PPAR Gamma Agonist + simvaststin Glaxosmithkline 3
MCC-555, Netoglitazone Mitsubishi Pharma, Novartis  
Muraglitzar Bristol-Myers Squibb 3
R483 Roche 2
PPM-204 Wyeth, Plexxikon 2

Oral glucokinase activator (GKA)
PSN010 OSI 1
R1511 Roche 1
G protein-coupled Receptor(GPR) 119 Agonist
PSN821 OSI  
Antisense drug for Glucagon Receptor (GCGR)
ISIS 325568 Isis 1
Antisense drug for Glucocorticoid Receptor (GCCR)
ISIS 377131 Isis Preclinical
Sodium Glucose Transporter 2 (SGLT2) inhibitor
AVE2268 Sanofi Aventis 2
SAR 7226 Sanofi Aventis Preclinical
189075 Glaxosmithkline 2
869682 Glaxosmithkline 2
Growth hormone releasing analogue
TH 9507 Theratechnolgies  
Nitric oxide (NO) blocking agent
NOX-700 Medinox 1 staretd in 2002
Selective inhibitor of fructose-1, 6-bisphosphatase (FBPase)
CS-917 Sankyo,Metabasis 2
MB07803 metabasis, Daiichi Sankyo 2
11-beta hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitor
AMG 221 Amgen, Biovitrum 1
Polypyrimidine tract binding protein (PTB, also named hnRNP) inhibitor
  Serono 1
Insulin Like Growth Factor 1
IPLEX (Mecasermin rinfabate) Glen Allen Orphan Drug Status
Newer Meglitinides
Nateglinide with insulin sensitizers Astellas pharmas SNDA Filed
Nateglinide with biguanides Astellas pharmas SNDA Filed
Islet Regeneration Factors
DG770 (beta cell regeneration factor) Develogen AG 3
E1 INT (Islet regeneration) Transition Therapeutics 2

AMG 837 (Potentiates Glucose Dependent Insulin Secretion) Amgen 1
MBX 213 Metabolex 1
R 1499 Roche 1
R1438 Roche 2
R1440 Roche 2
PSN 357 OSI 1
NBI 6024 Neurocrine Biosciences 2
MK 0941 Merck 1
MK 1642 Merck 1
Mk 0533 Merck 2
MK0893 Merck 2
Oral Insulin Emisphere Technologies 2
Technosphere Mannkind corporation 3
NN344 (Insulin analogue) Novo Nordisk 1
NN5401(Insulin analogue) Novo Nordisk 1
AERx® iDMS (Insulin Inhalation system) Novo Nordisk 3
Inhaled insulin Bristol Meyers Squibb 1
Inhaled insulin Eli Lilly 2
Exubera (Inhaled insulin) Pfizer 4
Oal Lyn (Inhaled insulin) http://www.generex.com/products/oral-lyn/ Approved in Ecuador
Nasulin Bentley 2

Product Pathways

Product pipeline

Intellectual Property

Search strategy

  • Database/Vendor: Micropat
  • Search scope: US Granted US Applications EP-A EP-B WO JP (bibliographic data only) DE-C,B DE-A DE-T DE-U GB-A FR-A; English Title
  • Years: Issue/Publication Date: >20051231
  • Search String: (Diabetes OR diabetic) AND (treatment OR treating)
  • Hits: 618/217 patents (with/with out family members)
  • Date of search: 11 July 2007

Top players and IPC classes

Diabetes- top players.jpeg

IPC code definition

A61K Preparations for medical, dental, or toilet purposes
C07D Heterocyclic compounds
C07K Peptides
C12N Micro-organisms or enzymes; compositions thereof
C12Q Measuring or testing processes involving enzymes or micro-organisms (immunoassay); compositions or test papers therefor; processes of preparing such compositions; condition-responsive control in microbiological or enzymological processes

Geographical Distribution and Treatment Approaches

Diabetes -geographical.jpeg

IP activity and Treatment Approaches

  • Decline in the IP activity during 2005 and 2006 is due 18 months publication delay of patent document.
Diabetes -year approach.jpeg

Clinical Trials


Clinical trials
Drug Sponsors Description Phase Date of Start
Oral Drugs
Cannabinoid receptor antagonist
Rimonabant Sanofi-Aventis The primary objective of this study is to assess the efficacy of SR141716 (rimonabant) compared to placebo on change in HbA1c and on relative change in body weight over 52 weeks in obese type 2 diabetic patients on monotherapy inadequately controlled with oral anti-diabetic drug (sulfonylurea or ?-glucosidase inhibitor). 3 May-07
Insulin Sensitisers
Metaglidasen Metabolex 2, 3 May-06
Rosiglitazone maleate/metformin hydrochloride (AVANDAMET) GlaxoSmithKline This study will evaluate the longer-term glycemic effect of two medicines approved for initial treatment of type 2 diabetes. 4 Oct-06
Balaglitazone Rheoscience A/S Balaglitazone is a thiazolidinedione derivative that is being developed as an oral anti-diabetic drug to improve blood glucose control in patients with type 2 diabetes. The purpose of this study is to assess if additional treatment with balaglitazone in patients with type 2 diabetes on stable insulin treatment will improve blood glucose control and decrease the daily insulin dose, but with less impact on weight gain and oedema. 3 Jul-07
(DPP-4) inhibitor
Vildagliptin Novartis This is a 24-week study to assess the efficacy on HbA1c of 100 mg vildagliptin once daily as compared to placebo as add-on to metformin in patients with type 2 diabetes inadequately controllled with metformin. 3 May-06
Oral Insulin NIDDK, NICHD, NIAID, NICR, ADA, JDRF N/A 3 Feb-07
Potassium Channel Blocker
Diazoxide Grill, Valdemar, M.D. The purpose of this study is to find out if Diazoxide can partly retain insulin production in newly diagnosed type 1 diabetes patients. 4 Feb-05
Nutritional Agents
Benfotiamine (Vitamin B1) University Hospital, Aker, The Research Council of Norway N/A 1, 2 Aug-05
Docosahexaenoic acid (DHA) NIDDK N/A 2 June 2006
Vitamin D University of Tromso The purpose of the study is to evaluate if supplementation with vitamin D in a dose of 40.000 IU per week will result in improved metablic control in patients with type 2 diabetes. 2 Jun-06
Carnitine Supplementation Childrens Mercy Hospital Kansas City,Sigma Tau Pharmaceuticals, Inc, Minimed Pharmaceuticals, Pharmacia/Upjohn Career Development Award The purpose of this study is to determine whether type I diabetics with carnitine deficiency exhibit increased numbers of hypoglycemic (low blood sugars) events and if unrecognized hypoglycemia occurs during continuous 72-hour glucose monitoring. If they are determined to have unrecognized hypoglycemia, then oral carnitine supplementation will be given to those subjects and they will be reassessed for the number of hypoglycemic events in a 72-hour glucose monitoring. Oct-04
Salsalate NIDDK,National Institutes of Health Clinical Center This study, conducted at the Phoenix Indian Medical Center, Phoenix, Arizona, will determine whether reducing subclinical inflammation lessens insulin resistance in healthy, obese volunteers. 4 Mar-03
Angiotensin (AT 2) Antagonist/blocker
Olmesartan Daiichi Sankyo Inc N/A 3 Oct-04
MBX-2044 Metabolex The purpose of this study is to collect important information regarding the glucose-lowering efficacy of MBX-2044 and the safety of MBX-2044 (especially weight gain and edema) in diabetics. It will also provide important information about the appropriate doses to be used in subsequent longer-term studies to evaluate the safety and efficacy of MBX-2044 alone and in combination with other anti-diabetic agents. 2 Oct-06
PF-00734200 Pfizer The purpose of this Phase 2a study is to evaluate the efficacy, safety and tolerability, of multiple parallel doses of PF-00734200 following oral administration to adult human subjects with T2DM who currently are on a stable dose of metformin. 2 Jun-07
CP-945,598 Pfizer The purpose of this study is to determine if CP-945,598 is effective in the treatment of obesity in type 2 diabetic patients 3 Nov-06
WelChol® (colesevelam) Daiichi Sankyo Inc This study is designed to assess the potential mechanism of action by which WelChol® (colesevelam) may improve blood glucose control in patients with type 2 diabetes 2 May-05
Aleglitazar and Actos® Hoffmann-La Roche This study will compare the effects of aleglitazar and Actos®, added to preexisting oral antihyperglycemic therapy and/or diet and exercise, on renal function in patients with type 2 diabetes, and normal or mildly impaired renal function. 2 June 2007
BI 1356 BS Boehringer Ingelheim Pharmaceuticals The objective of this monotherapy study is to investigate the efficacy, safety, and tolerability of 3 doses of BI 1356 BS compared to placebo over 12 weeks of treatment in patients with type 2 diabetes and insufficient control of thier blood glucose. In addition, there will be an open-label treatment arm with metformin. The hypothesis of the trial is that the test drug, BI 1356 BS will lead to better control of blood glucose compared to placebo after 12 weeks of treatment. 2 May-06
BMS-512148 Bristol-Myers Squibb The purpose of this clinical research study is to learn if BMS-512148, added to insulin and one or two anti-diabetes medications (metformin and/or pioglitazone or rosiglitazone), can help reduce the blood sugar levels compared to insulin and one or two anti-diabetes medications (metformin and/or pioglitazone or rosiglitazone) alone, in subjects with type 2 diabetes. 2, 3 October 2006
Parenteral routes
Insuline glargine Sanofi-Aventis Purpose ogf this study is to determine rhe first dose and titration of basal insulin 4 May-06
Basal Insulin Plus Insulin Glulisine Sanofi-Aventis To evaluate the efficacy of a single injection of glulisine before the main meal added to insulin glargine plus oral antidiabetic drugs (OADs) compared to insulin glargine plus OADs in Type 2 diabetic patients poorly controlled with basal insulin plus OADs. 4 Jul-06
Inhaled Insulin (Exubera) Pfizer To assess the impact on glucose control by inhaled insulin in patients with type 2 diabetes who are not well controlled on 2 or more oral anti-diabetic agents 3 Mar-06
Insulin Inhalation Powder Eli Lilly and Company This is a phase 3, open-label, randomized study to evaluate the safety and efficacy of the Lilly/Alkermes inhaled insulin system compared to injected pre-meal insulin in non-smoking patients with type 2 diabetes. Patients will be treated for 24 months with a 2-month follow-up period. 3 Apr-06
Levemir Novo Nordisk This trial aims for a comparison of the effect on glycaemic control in subjects with type 2 diabetes under both established Western algorithm and Korean practical algorithm, given in combination with oral diabetic drug(s) 4 Aug-07
Pulsatile IV Insulin Florida Atlantic University The purpose of this study is to determine if restoring normal metabolic function in patients with either type I or type II diabetes can improve the impact of the consequences of diabetic complications on the overall quality of life of diabetic patients. Patients are treated once a week with pulsatile intravenous insulin therapy mimicking normal insulin secretion. 2, 3 Mar-03
Incretin Minetic
Exenatide With Basal Insulin Amylin Pharmaceuticals, Eli Lilly This is a phase 3 trial designed to compare the effects of twice daily exenatide plus oral antidiabetic agents (OADs) and once-daily insulin glargine plus OADs with respect to glycemic control, as measured by hemoglobin A1c, with minimum weight gain, in patients with uncontrolled type 2 diabetes on OADs. 3 Jun-06
Exenatide Baylor College of Medicine, NIH The purpose of this study is to see if giving exenatide and insulin before a meal would lower blood sugars after the meal. 4 Mar-07
Exenatide Plus Metformin vs. Insulin Aspart Plus Metformin Amylin Pharmaceuticals, Eli Lilly This study in Germany is designed to compare the effects of twice-daily exenatide plus metformin and twice-daily premixed human insulin aspart plus metformin with respect to glycemic control, as measured by HbA1c, combined with the percentage of patients with at least one treatment-emergent hypoglycemic episode. Patients will be treated with study therapy for approximately 26 weeks. 3 Feb-07
Sitigliptin Merck Frosst Canada Ltd, University of British Columbia 2 Nov-06
hOKT3gamma1 (Ala-Ala) NIAID hOKT3gamma1 (Ala-Ala) is a man-made antibody that is commonly used to prevent organ rejection. The purpose of this study is determine whether hOKT3gamma1 (Ala-Ala) can halt the progression of newly diagnosed type 1 diabetes. 2 Sep-05
Anti-CD20 (rituximab) NIDDK, NICHD, NIAID, NICR, ADA, JDRF This study will investigate the use of rituximab to see if it can help lower the number of immune B cells thereby preventing the destruction of any remaining insulin producing beta cells that remain at diagnosis. 2, 3 Dec-06
Islet Cell Transplants Weill Medical College of Cornell University 1 Aug-03


Conference Update: American Diabetic Association 2007

Conference highlights for Oral Hypoglycemic Agents

  1. Oral hypoglecemic agents and their role in diabetes treatment. The focus was the recent meta analysis published in NEJM, showing increase CV mortality with Rosiglitazone. The panel consensus was that while awaiting more safety data, for now those patients who are tolerating Rosiglitazone should continue taking them, whereas newly diagnosed patients should try alternative treatment. Also all PPAR agonists should be treated as distinct entities rather than having class effect.
  2. 12 different diabetes products are in various stages of development, and there were about 55 abstracts talking about DPP–IV inhibitors. They are especially useful for:
    • The elderly
    • Those with renal insufficiency
    • Heart failure patients
  3. Amyline analogue (Pramlinitide) was combined with Insulin for treatment of Type 2 DM and results were favorable.
  4. Continuous glucose monitoring using implanted glucose sensors is a step forward in evolving technology. Yet it is still very expensive and best for highly trained patients on intensive insulin therapy.

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