Safety, Tolerability and Pharmacokinetics Study of EGT0001474 in Subjects With Type 2 Diabetes

NCT ID: NCT00924053

Last Updated: 2019-06-17

Study Results

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Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE1

Total Enrollment

24 participants

Study Classification

INTERVENTIONAL

Study Start Date

2009-06-30

Study Completion Date

2009-07-31

Brief Summary

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The purpose of this study is to determine the safety, tolerability and pharmacokinetics (how much of the drug gets into the blood and how long it takes the body to get rid of it) of single doses of EGT0001474 given to patients with Type 2 diabetes. The study will also evaluate how EGT0001474 affects the amount of glucose produced by the body in the urine.

Detailed Description

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EGT0001474 is a compound that may inhibit the effect of other compounds in the body known as sugar transporters. The use of EGT0001474 may enhance the elimination of glucose from the blood by increasing the amount of urine produced. This would help prevent an abnormal decrease in blood sugar (hypoglycemia) both during fasting and after meals without increasing insulin secretion (which may result in weight gain or an abnormal increase in blood sugar known as Type 2 diabetes).

Conditions

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Diabetes Mellitus Type 2

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

QUADRUPLE

Participants Caregivers Investigators Outcome Assessors

Study Groups

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EGT0001474

Group Type EXPERIMENTAL

EGT0001474

Intervention Type DRUG

Cohort 1: single dose of 25 mg EGT0001474 given as an oral capsule; Cohort 2: single dose of 75 mg EGT0001474 given as 3 oral capsules; Cohort 3: single dose of 150 mg EGT0001474 given as 6 oral capsules.

Placebo

Group Type PLACEBO_COMPARATOR

Placebo

Intervention Type DRUG

Placebo capsules to match EGT0001474

Interventions

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EGT0001474

Cohort 1: single dose of 25 mg EGT0001474 given as an oral capsule; Cohort 2: single dose of 75 mg EGT0001474 given as 3 oral capsules; Cohort 3: single dose of 150 mg EGT0001474 given as 6 oral capsules.

Intervention Type DRUG

Placebo

Placebo capsules to match EGT0001474

Intervention Type DRUG

Other Intervention Names

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Human SGLT2 inhibitor Human SGLT2 inhibitor

Eligibility Criteria

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Inclusion Criteria

* Male or females between the ages of 18 to 70 diagnosed with Type 2 diabetes.
* Body mass Index (BMI) between 18 kg/m2 and 37 kg/m2.
* HbA1c levels between 6.5 and 9.0 (inclusive) where the upper limit of normal for the HbA1c assay is 6.4% or 6.2-9.0% (inclusive) where the upper limit of normal for the HbA1c assay is 6.1% and fasting plasma glucose between 110 and 240 mg/dL (inclusive) while on diabetic medications.
* If taking drugs for diabetes, must be medically able and willing to discontinue diabetes medications for the duration of the study.
* Female subjects must be surgically sterilized or postmenopausal.
* Non-smoker for at least 3 months.
* Negative alcohol screen.

Exclusion Criteria

* Type 1 diabetes.
* Use of insulin therapy or oral antidiabetic medication other than metformin, sitagliptin or a sulfonylurea.
* Sitting blood pressure above 150/95 mmHg on 2 evaluations at least 10 minutes apart at screening.
* Treatment with an investigational drug within 30 days or 7 half-lives, whichever is longer.
* Previous treatment with EGT0001474.
* Vaccination within 30 days prior to the first dose of study medication.
Minimum Eligible Age

18 Years

Maximum Eligible Age

70 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Theracos

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Mason W. Freeman, M.D.

Role: STUDY_CHAIR

Massachusetts General Hospital

Locations

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dgd Research Inc., a Cetero Research Company

San Antonio, Texas, United States

Site Status

Countries

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United States

References

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Blondel O, Bailbe D, Portha B. Insulin resistance in rats with non-insulin-dependent diabetes induced by neonatal (5 days) streptozotocin: evidence for reversal following phlorizin treatment. Metabolism. 1990 Aug;39(8):787-93. doi: 10.1016/0026-0495(90)90120-2.

Reference Type BACKGROUND
PMID: 2198430 (View on PubMed)

Cowie CC, Rust KF, Byrd-Holt DD, Eberhardt MS, Flegal KM, Engelgau MM, Saydah SH, Williams DE, Geiss LS, Gregg EW. Prevalence of diabetes and impaired fasting glucose in adults in the U.S. population: National Health And Nutrition Examination Survey 1999-2002. Diabetes Care. 2006 Jun;29(6):1263-8. doi: 10.2337/dc06-0062.

Reference Type BACKGROUND
PMID: 16732006 (View on PubMed)

American Diabetes Association. Economic costs of diabetes in the U.S. In 2007. Diabetes Care. 2008 Mar;31(3):596-615. doi: 10.2337/dc08-9017.

Reference Type BACKGROUND
PMID: 18308683 (View on PubMed)

American Diabetes Association. Standards of medical care in diabetes--2008. Diabetes Care. 2008 Jan;31 Suppl 1:S12-54. doi: 10.2337/dc08-S012. No abstract available.

Reference Type BACKGROUND
PMID: 18165335 (View on PubMed)

Ehrenkranz JR, Lewis NG, Kahn CR, Roth J. Phlorizin: a review. Diabetes Metab Res Rev. 2005 Jan-Feb;21(1):31-8. doi: 10.1002/dmrr.532.

Reference Type BACKGROUND
PMID: 15624123 (View on PubMed)

Han S, Hagan DL, Taylor JR, Xin L, Meng W, Biller SA, Wetterau JR, Washburn WN, Whaley JM. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes. 2008 Jun;57(6):1723-9. doi: 10.2337/db07-1472. Epub 2008 Mar 20.

Reference Type BACKGROUND
PMID: 18356408 (View on PubMed)

Jabbour SA, Goldstein BJ. Sodium glucose co-transporter 2 inhibitors: blocking renal tubular reabsorption of glucose to improve glycaemic control in patients with diabetes. Int J Clin Pract. 2008 Aug;62(8):1279-84. doi: 10.1111/j.1742-1241.2008.01829.x.

Reference Type BACKGROUND
PMID: 18705823 (View on PubMed)

Komoroski B, Vachharajani N, Feng Y, Li L, Kornhauser D, Pfister M. Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus. Clin Pharmacol Ther. 2009 May;85(5):513-9. doi: 10.1038/clpt.2008.250. Epub 2009 Jan 7.

Reference Type BACKGROUND
PMID: 19129749 (View on PubMed)

Krook A, Kawano Y, Song XM, Efendic S, Roth RA, Wallberg-Henriksson H, Zierath JR. Improved glucose tolerance restores insulin-stimulated Akt kinase activity and glucose transport in skeletal muscle from diabetic Goto-Kakizaki rats. Diabetes. 1997 Dec;46(12):2110-4. doi: 10.2337/diab.46.12.2110.

Reference Type BACKGROUND
PMID: 9392506 (View on PubMed)

Oku A, Ueta K, Arakawa K, Ishihara T, Nawano M, Kuronuma Y, Matsumoto M, Saito A, Tsujihara K, Anai M, Asano T, Kanai Y, Endou H. T-1095, an inhibitor of renal Na+-glucose cotransporters, may provide a novel approach to treating diabetes. Diabetes. 1999 Sep;48(9):1794-800. doi: 10.2337/diabetes.48.9.1794.

Reference Type BACKGROUND
PMID: 10480610 (View on PubMed)

Pajor AM, Wright EM. Cloning and functional expression of a mammalian Na+/nucleoside cotransporter. A member of the SGLT family. J Biol Chem. 1992 Feb 25;267(6):3557-60.

Reference Type BACKGROUND
PMID: 1740408 (View on PubMed)

Santer R, Kinner M, Lassen CL, Schneppenheim R, Eggert P, Bald M, Brodehl J, Daschner M, Ehrich JH, Kemper M, Li Volti S, Neuhaus T, Skovby F, Swift PG, Schaub J, Klaerke D. Molecular analysis of the SGLT2 gene in patients with renal glucosuria. J Am Soc Nephrol. 2003 Nov;14(11):2873-82. doi: 10.1097/01.asn.0000092790.89332.d2.

Reference Type BACKGROUND
PMID: 14569097 (View on PubMed)

Toggenburger G, Kessler M, Semenza G. Phlorizin as a probe of the small-intestinal Na+,D-glucose cotransporter. A model. Biochim Biophys Acta. 1982 Jun 14;688(2):557-71. doi: 10.1016/0005-2736(82)90367-4.

Reference Type BACKGROUND
PMID: 7201854 (View on PubMed)

Tsujihara K, Hongu M, Saito K, Inamasu M, Arakawa K, Oku A, Matsumoto M. Na(+)-glucose cotransporter inhibitors as antidiabetics. I. Synthesis and pharmacological properties of 4'-dehydroxyphlorizin derivatives based on a new concept. Chem Pharm Bull (Tokyo). 1996 Jun;44(6):1174-80. doi: 10.1248/cpb.44.1174.

Reference Type BACKGROUND
PMID: 8814948 (View on PubMed)

Other Identifiers

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THR-1474-C-396

Identifier Type: -

Identifier Source: org_study_id

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