Bexagliflozin

Bexagliflozin
Clinical data
Trade names	Brenzavvy, Bexacat
AHFS/Drugs.com	Monograph
MedlinePlus	a623027
License data	US DailyMed: Bexagliflozin;
Routes of; administration	By mouth
ATC code	A10BK08 (WHO) QA10BK08 (WHO);
Legal status
Legal status	US: ℞-only;
Identifiers
	IUPAC name (2S,3R,4R,5S,6R)-2-[4-Chloro-3-[[4-(2-cyclopropyloxyethoxy)phenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol;
CAS Number	1118567-05-7;
PubChem CID	25195624;
DrugBank	DB12236;
ChemSpider	26609013;
UNII	EY00JF42FV;
KEGG	D10865;
ChEBI	CHEBI:229225;
ChEMBL	ChEMBL1808388;
Chemical and physical data
Formula	C24H29ClO7
Molar mass	464.94 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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]

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

Legal status

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]

References

^ ^a ^b "Bexacat- bexagliflozin tablets tablet". DailyMed. 16 January 2023. Archived from the original on 21 January 2023. Retrieved 21 January 2023.
^ ^a ^b ^c ^d ^e ^f ^g "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. This article incorporates text from this source, which is in the public domain.
^ ^a ^b ^c ^d "Brenzavvy- bexagliflozin tablet". DailyMed. 18 September 2023. Archived from the original on 20 November 2023. Retrieved 20 November 2023.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p "Drug Trials Snapshots: Brenzavvy". U.S. Food and Drug Administration (FDA). 16 February 2024. Retrieved 14 March 2024. This article incorporates text from this source, which is in the public domain.
^ ^a ^b "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. This article incorporates text from this source, which is in the public domain.
^ "Drug Approval Package: Brenzavvy". U.S. Food and Drug Administration (FDA). 21 February 2023. Retrieved 14 March 2024.
^ 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.
^ 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.
^ 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.
^ ^a ^b "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.

External links

Clinical trial number NCT02715258 for "Safety and Efficacy of Bexagliflozin as Monotherapy in Patients With Type 2 Diabetes" at ClinicalTrials.gov
Clinical trial number NCT03259789 for "Safety and Efficacy of Bexagliflozin Compared to Placebo as Add-on Therapy to Metformin in Type 2 Diabetes Subjects" at ClinicalTrials.gov
Clinical trial number NCT02769481 for "Safety and Efficacy of Bexagliflozin Compared to Glimepiride as Add-on Therapy to Metformin in Type 2 Diabetes Subjects" at ClinicalTrials.gov
Clinical trial number NCT03115112 for "Safety and Efficacy of Bexagliflozin Compared to Sitagliptin as Add-on Therapy to Metformin in Type 2 Diabetes Subjects" at ClinicalTrials.gov
Clinical trial number NCT02836873 for "Safety and Efficacy of Bexagliflozin in Type 2 Diabetes Mellitus Patients With Moderate Renal Impairment" at ClinicalTrials.gov
Clinical trial number NCT02558296 for "Bexagliflozin Efficacy and Safety Trial (BEST)" at ClinicalTrials.gov

[Bexacat_FDA_label-1] "Bexacat- bexagliflozin tablets tablet". DailyMed. 16 January 2023. Archived from the original on 21 January 2023. Retrieved 21 January 2023.

[FDA_Bexagliflozin-2] ^ ^a ^b ^c ^d ^e ^f ^g "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. This article incorporates text from this source, which is in the public domain.

[Brenzavvy_FDA_label-3] "Brenzavvy- bexagliflozin tablet". DailyMed. 18 September 2023. Archived from the original on 20 November 2023. Retrieved 20 November 2023.

[Brenzavvy_FDA_snapshot-4] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p "Drug Trials Snapshots: Brenzavvy". U.S. Food and Drug Administration (FDA). 16 February 2024. Retrieved 14 March 2024. This article incorporates text from this source, which is in the public domain.

[Novel_Drug_Approvals_for_2023-5] "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. 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.

[Halvorsen-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.

[Halvorsen_et_al.-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.

[Allegretti_et_al.-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.

[Elanco_PR-10] "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.

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