Bexagliflozin

Last updated

Bexagliflozin
Bexagliflozin structure.svg
Clinical data
Trade names Brenzavvy, Bexacat
AHFS/Drugs.com Monograph
MedlinePlus a623027
License data
Routes of
administration 		By mouth
ATC code
Legal status
Legal status
Identifiers
  • (2S,3R,4R,5S,6R)-2-[4-Chloro-3-[[4-(2-cyclopropyloxyethoxy)phenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
Formula C24H29ClO7
Molar mass 464.94 g·mol−1
3D model (JSmol)
  • C1CC1OCCOC2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)Cl
  • InChI=1S/C24H29ClO7/c25-19-8-3-15(24-23(29)22(28)21(27)20(13-26)32-24)12-16(19)11-14-1-4-17(5-2-14)30-9-10-31-18-6-7-18/h1-5,8,12,18,20-24,26-29H,6-7,9-11,13H2/t20-,21-,22+,23-,24+/m1/s1
  • Key:BTCRKOKVYTVOLU-SJSRKZJXSA-N

Bexagliflozin, sold under the brand name Brenzavvy, is an antidiabetic medication used to improve glycemic control in adults with type 2 diabetes. [3] [4] It is a sodium-glucose cotransporter 2 (SGLT2) inhibitor that is taken by mouth. [1] [2]

Contents

The most common side effects include genital yeast infections, urinary tract infections, and increased urination. [4]

Bexagliflozin was approved for medical use in the United States in January 2023. [4] [5]

Medical uses

Bexagliflozin is indicated to improve glycemic control in adults with type 2 diabetes in combination with diet and exercise. [3] [4] [5]

Adverse effects

Bexagliflozin may cause ketoacidosis, a serious, potentially life-threatening complication that occurs when the body produces high levels of acids in the blood. [4] Bexagliflozin may also cause serious side effects such as an increased incidence for surgery to remove parts of the legs or feet, decreases in blood pressure due to excessive loss of water and sodium from the body, serious infections in the genital region (Fournier’s gangrene), very low blood sugar levels when used in combination with insulin or medications that increase insulin in the body, and serious urinary tract infections. [4]

History

The US Food and Drug Administration (FDA) approved bexagliflozin based on evidence from nine clinical trials that enrolled 4,462 adults (2,578 of these participants received bexagliflozin). [4] The nine trials were conducted at 428 sites in 16 countries including the United States, Mexico, Colombia, Japan, the Czech Republic, Poland, Spain, Hungary, France, Canada, Netherlands, Denmark, South Korea, Taiwan, Russia, and Germany. [4] All nine trials were used to assess safety and six of these trials (enrolling 3,346 participants of the 4,462 participants) were used to assess the efficacy of bexagliflozin. [4] The efficacy of bexagliflozin was evaluated in six clinical trials, while the safety of bexagliflozin was evaluated in nine clinical trials of adults with type 2 diabetes whose blood sugar was not well controlled. [4] All participants were required to follow diet and exercise recommendations, but the trials differed with respect to which other drugs participants were allowed to use for diabetes treatment. [4] In four trials, participants were randomly assigned to receive either bexagliflozin or placebo by mouth once daily. [4] In two trials, they received either bexagliflozin or a different diabetes medicine. [4] Neither the participants nor the healthcare providers knew which treatment participants received until after the trial was completed. [4] The benefit of bexagliflozin was evaluated by the change in hemoglobin A1c (HbA1c) between the bexagliflozin and the comparator (either placebo or another diabetes medicine) at the end of the treatment period. [4]

Society and culture

Bexagliflozin was approved for medical use in the United States in January 2023. [3] [4] [6]

Research

A 96-week phase II clinical study of adults with type 2 diabetes showed that bexagliflozin monotherapy provided a durable, clinically meaningful improvement of glycemic control, with a substantial reduction in weight and blood pressure, but no increase in the rate of significant adverse events. [7] [8] In a clinical study of patients with type 2 diabetes and stage 3a/3b chronic kidney disease, bexagliflozin was well tolerated and shown to reduce hemoglobin A1c levels, body weight, systolic blood pressure and albuminuria. [9]

Veterinary uses

The data from two six-month field studies and an extended use field study demonstrated that bexagliflozin was over 80% effective in improving glycemic control in cats with diabetes mellitus. [2]

Bexagliflozin, sold under the brand name Bexacat, is an antidiabetic medication used to improve glycemic control in cats with diabetes. [2] Bexacat is the first sodium-glucose cotransporter 2 (SGLT2) inhibitor new animal drug approved by the US Food and Drug Administration (FDA) in any animal species. [2] It was approved for medical use in the United States in December 2022. [2] [10] Bexacat is sponsored by Increvet Inc., based in Boston, Massachusetts. [2] Elanco licensed development and commercialization rights for bexagliflozin from Bexcafe, an affiliate of Increvet. [10]

Related Research Articles

Drugs used in diabetes treat diabetes mellitus by decreasing glucose levels in the blood. With the exception of insulin, most GLP-1 receptor agonists, and pramlintide, all diabetes medications are administered orally and are thus called oral hypoglycemic agents or oral antihyperglycemic agents. There are different classes of hypoglycemic drugs, and selection of the appropriate agent depends on the nature of diabetes, age, and situation of the person, as well as other patient factors.

<span class="mw-page-title-main">Sitagliptin</span> Diabetes medication

Sitagliptin, sold under the brand name Januvia among others, is an anti-diabetic medication used to treat type 2 diabetes. In the United Kingdom it is listed as less preferred than metformin or a sulfonylurea. It is taken by mouth. It is also available in the fixed-dose combination medication sitagliptin/metformin.

<span class="mw-page-title-main">Saxagliptin</span> Chemical compound

Saxagliptin, sold under the brand name Onglyza, is an oral hypoglycemic of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. Early development was solely by Bristol-Myers Squibb; in 2007 AstraZeneca joined with Bristol-Myers Squibb to co-develop the final compound and collaborate on the marketing of the drug.

<span class="mw-page-title-main">Dapagliflozin</span> Diabetes medication

Dapagliflozin, sold under the brand names Farxiga (US) and Forxiga (EU) among others, is a medication used to treat type 2 diabetes. It is also used to treat adults with heart failure and chronic kidney disease. It reversibly inhibits sodium-glucose co-transporter 2 (SGLT-2) in the renal proximal convoluted tubule to reduce glucose reabsorption and increase urinary glucose excretion.

<span class="mw-page-title-main">Muraglitazar</span> Chemical compound

Muraglitazar is a dual peroxisome proliferator-activated receptor agonist with affinity to PPARα and PPARγ.

<span class="mw-page-title-main">Remogliflozin etabonate</span> Chemical compound

Remogliflozin etabonate (INN/USAN) is a drug of the gliflozin class for the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin was discovered by the Japanese company Kissei Pharmaceutical and is currently being developed by BHV Pharma, a wholly owned subsidiary of North Carolina, US-based Avolynt, and Glenmark Pharmaceuticals through a collaboration with BHV. In 2002, GlaxoSmithKline (GSK) received a license to use it. From 2002 to 2009, GSK carried out a significant clinical development program for the treatment of type-2 diabetes mellitus in various nations across the world and obesity in the UK. Remogliflozin etabonate's pharmacokinetics, pharmacodynamics, and clinical dose regimens were characterized in 18 Phase I and 2 Phase II investigations. Due to financial concerns, GSK stopped working on remogliflozin and sergliflozin, two further SGLT2 inhibitors that were licensed to the company, in 2009. Remogliflozin was commercially launched first in India by Glenmark in May 2019.

<span class="mw-page-title-main">Canagliflozin</span> Chemical compound

Canagliflozin, sold under the brand name Invokana among others, is a medication used to treat type 2 diabetes. It is used together with exercise and diet. It is not recommended in type 1 diabetes. It is taken by mouth.

<span class="mw-page-title-main">Insulin degludec</span> Ultralong-acting basal insulin analogue

Insulin degludec (INN/USAN) is an ultralong-acting basal insulin analogue that was developed by Novo Nordisk under the brand name Tresiba. It is administered via subcutaneous injection to help control the blood sugar level of those with diabetes. It has a duration of action that lasts up to 42 hours, making it a once-daily basal insulin, that is one that provides a base insulin level, as opposed to the fast- and short-acting bolus insulins.

Sitagliptin/metformin, sold under the brand name Janumet among others, is a fixed-dose combination anti-diabetic medication used to treat type 2 diabetes. It may be used in those whose blood sugar is not controlled with metformin and a sulfonylurea. It is taken by mouth.

<span class="mw-page-title-main">Gemigliptin</span> Chemical compound

Gemigliptin (rINN), sold under the brand name Zemiglo, is an oral anti-hyperglycemic agent of the dipeptidyl peptidase-4 inhibitor class of drugs. Glucose lowering effects of DPP-4 inhibitors are mainly mediated by GLP-1 and gastric inhibitory polypeptide (GIP) incretin hormones which are inactivated by DPP-4.

Empagliflozin, sold under the brand name Jardiance, among others, is an antidiabetic medication used to improve glucose control in people with type 2 diabetes. It is not recommended for type 1 diabetes. It is taken by mouth.

<span class="mw-page-title-main">Dulaglutide</span> Diabetes medication

Dulaglutide, sold under the brand name Trulicity among others, is a medication used for the treatment of type 2 diabetes in combination with diet and exercise. It is also approved in the United States for the reduction of major adverse cardiovascular events in adults with type 2 diabetes who have established cardiovascular disease or multiple cardiovascular risk factors. It is a once-weekly injection.

Gliflozins are a class of drugs in the treatment of type 2 diabetes (T2D). They act by inhibiting sodium/glucose cotransporter 2 (SGLT-2), and are therefore also called SGLT-2 inhibitors. The efficacy of the drug is dependent on renal excretion and prevents glucose from going into blood circulation by promoting glucosuria. The mechanism of action is insulin independent.

SGLT2 inhibitors are a class of medications that inhibit sodium-glucose transport proteins in the nephron, unlike SGLT1 inhibitors that perform a similar function in the intestinal mucosa. The foremost metabolic effect of this is to inhibit reabsorption of glucose in the kidney and therefore lower blood sugar. They act by inhibiting sodium/glucose cotransporter 2 (SGLT2). SGLT2 inhibitors are used in the treatment of type 2 diabetes. Apart from blood sugar control, gliflozins have been shown to provide significant cardiovascular benefit in people with type 2 diabetes. As of 2014, several medications of this class had been approved or were under development. In studies on canagliflozin, a member of this class, the medication was found to enhance blood sugar control as well as reduce body weight and systolic and diastolic blood pressure.

<span class="mw-page-title-main">Ipragliflozin</span> Chemical compound

Ipragliflozin is a pharmaceutical drug for treatment of type 2 diabetes. Ipragliflozin, jointly developed by Astellas Pharma and Kotobuki Pharmaceutical, was approved in Japan on January 17, 2014, and in Russia on May 22, 2019.

<span class="mw-page-title-main">Gosogliptin</span> Chemical compound

Gosogliptin is a drug for the treatment of type II diabetes. It is in the class of dipeptidyl peptidase-4 (DPP-4) inhibitors. It was discovered and developed through Phase 1 and Phase 2 by Pfizer. The crystal structure of DPP-4 in complex with gosogliptin is available. Its metabolism, excretion and pharmacokinetics in rat, dog and human have been described. A cost efficient route has been published. Other studies including Phase 3 studies were conducted in Russia. It is approved for use in Russia.

<span class="mw-page-title-main">Ertugliflozin</span> Chemical compound

Ertugliflozin, sold under the brand name Steglatro, is a medication for the treatment of type 2 diabetes.

Dapagliflozin/metformin, sold under the brand name Xigduo XR amongst others, is a fixed-dose combination anti-diabetic medication used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It is a combination of dapagliflozin and metformin and is taken by mouth. Dapagliflozin/metformin was approved for use in the European Union in January 2014, in the United States in February 2014, and in Australia in July 2014.

<span class="mw-page-title-main">Tirzepatide</span> Anti-diabetic medication

Tirzepatide, sold under the brand name Mounjaro among others, is an antidiabetic medication used for the treatment of type 2 diabetes and for weight loss. Tirzepatide is administered via subcutaneous injections.

<span class="mw-page-title-main">Janagliflozin</span> Chemical compound

Janagliflozin is an SGLT2 inhibitor developed by Sihuan Pharmaceutical. It is approved in China for the treatment of type 2 diabetes.

References

  1. 1 2 "Bexacat- bexagliflozin tablets tablet". DailyMed. 16 January 2023. Archived from the original on 21 January 2023. Retrieved 21 January 2023.
  2. 1 2 3 4 5 6 7 "FDA Approves First Oral Treatment for Cats with Diabetes Mellitus". U.S. Food and Drug Administration (FDA). 8 December 2022. Archived from the original on 11 December 2022. Retrieved 11 December 2022.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  3. 1 2 3 4 "Brenzavvy- bexagliflozin tablet". DailyMed. 18 September 2023. Archived from the original on 20 November 2023. Retrieved 20 November 2023.
  4. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 "Drug Trials Snapshots: Brenzavvy". U.S. Food and Drug Administration (FDA). 16 February 2024. Retrieved 14 March 2024.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  5. 1 2 "Novel Drug Approvals for 2023". U.S. Food and Drug Administration (FDA). 20 January 2023. Archived from the original on 21 January 2023. Retrieved 21 January 2023.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  6. ↑ "Drug Approval Package: Brenzavvy". U.S. Food and Drug Administration (FDA). 21 February 2023. Retrieved 14 March 2024.
  7. ↑ Halvorsen YD, Lock JP, Frias JP, Tinahones FJ, Dahl D, Conery AL, et al. (September 2022). "A 96-week, double-blind, randomized controlled trial comparing bexagliflozin to glimepiride as an adjunct to metformin for the treatment of type 2 diabetes in adults". Diabetes, Obesity and Metabolism. 25 (1): 293–301. doi: 10.1111/dom.14875 . PMID   36178197. S2CID   252623503.
  8. ↑ Halvorsen YC, Walford GA, Massaro J, Aftring RP, Freeman MW (November 2019). "A 96-week, multinational, randomized, double-blind, parallel-group, clinical trial evaluating the safety and effectiveness of bexagliflozin as a monotherapy for adults with type 2 diabetes". Diabetes, Obesity and Metabolism. 21 (11): 2496–2504. doi:10.1111/dom.13833. PMID   31297965. S2CID   195892291.
  9. ↑ Allegretti AS, Zhang W, Zhou W, Thurber TK, Rigby SP, Bowman-Stroud C, et al. (September 2019). "Safety and effectiveness of bexagliflozin in patients with type 2 diabetes mellitus and stage 3a/3b CKD". American Journal of Kidney Diseases. 74 (3): 328–337. doi:10.1053/j.ajkd.2019.03.417. PMC   10077840 . PMID   31101403. S2CID   157066958.
  10. 1 2 "Elanco Announces FDA Approval of Bexacat (bexagliflozin tablets) – the First-of-its-Kind Oral Feline Diabetes Treatment Option" (Press release). Elanco. 9 December 2022. Archived from the original on 11 December 2022. Retrieved 11 December 2022.

Further reading

This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.