dapagliflozin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives 4304 461432-26-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dapagliflozin propanediol monohydrate
  • dapagliflozin propanediol
  • BMS 512148
  • forxiga
  • dapaglifozin
  • dapagliflozin
  • farxiga
  • dapagliflozin propylene glycolate hydrate
an Sodium-glucose cotransporter 2 (SGLT2) inhibitor, SGLT2 expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen, by inhibiting SGLT2, dapagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion
  • Molecular weight: 408.88
  • Formula: C21H25ClO6
  • CLOGP: 3.37
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 99.38
  • ALOGS: -3.37
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.70 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.09 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 12.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 12, 2012 EMA
Jan. 8, 2014 FDA ASTRAZENECA AB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diabetic ketoacidosis 2547.66 42.52 419 1488 3145 2353033
Ketoacidosis 881.61 42.52 141 1766 790 2355388
Fungal infection 398.18 42.52 95 1812 4794 2351384
Urinary tract infection 266.69 42.52 106 1801 29836 2326342
Weight decreased 173.41 42.52 77 1830 28294 2327884
Glycosylated haemoglobin increased 166.38 42.52 39 1868 1795 2354383
Dehydration 153.97 42.52 66 1841 22229 2333949
Blood glucose increased 146.49 42.52 54 1853 12236 2343942
Acute kidney injury 124.07 42.52 61 1846 28061 2328117
Metabolic acidosis 108.49 42.52 36 1871 5962 2350216
Ketonuria 96.43 42.52 16 1891 112 2356066
Hyperglycaemia 95.08 42.52 31 1876 4854 2351324
Pyelonephritis 91.68 42.52 25 1882 2116 2354062
Diabetes mellitus inadequate control 90.04 42.52 24 1883 1863 2354315
Hypoglycaemia 85.73 42.52 33 1874 8374 2347804
Candida infection 84.41 42.52 25 1882 2848 2353330
Product use issue 80.41 42.52 35 1872 12134 2344044
Vomiting 78.03 42.52 64 1843 71538 2284640
Cerebral infarction 73.72 42.52 25 1882 4412 2351766
Blood ketone body increased 73.63 42.52 12 1895 74 2356104
Sepsis 72.22 42.52 37 1870 18451 2337727
Euglycaemic diabetic ketoacidosis 71.58 42.52 13 1894 162 2356016
Dizziness 71.43 42.52 56 1851 58609 2297569
Urosepsis 65.95 42.52 19 1888 1962 2354216
Nausea 62.19 42.52 69 1838 112120 2244058
Pollakiuria 61.74 42.52 21 1886 3735 2352443
Polyuria 60.98 42.52 16 1891 1166 2355012
Malaise 59.00 42.52 49 1858 55536 2300642
Haematuria 58.88 42.52 21 1886 4297 2351881
Fournier's gangrene 52.16 42.52 8 1899 31 2356147
Vulvovaginal pruritus 51.70 42.52 12 1895 525 2355653
Thirst 50.87 42.52 15 1892 1679 2354499
Ketosis 50.75 42.52 9 1898 97 2356081
Pancreatitis 49.32 42.52 22 1885 8057 2348121
Off label use 49.02 42.52 50 1857 73548 2282630
Pyelonephritis acute 45.82 42.52 11 1896 557 2355621
Dysuria 45.65 42.52 17 1890 3924 2352254

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diabetic ketoacidosis 1930.17 46.68 356 1651 2927 1741847
Ketoacidosis 472.60 46.68 88 1919 707 1744067
Weight decreased 250.95 46.68 110 1897 22643 1722131
Dehydration 176.95 46.68 80 1927 17578 1727196
Glycosylated haemoglobin increased 172.28 46.68 45 1962 1846 1742928
Fournier's gangrene 158.69 46.68 28 1979 157 1744617
Urinary tract infection 158.21 46.68 63 1944 10090 1734684
Fungal infection 136.81 46.68 39 1968 2223 1742551
Balanoposthitis 133.66 46.68 26 1981 265 1744509
Blood glucose increased 128.58 46.68 55 1952 10529 1734245
Cerebral infarction 119.73 46.68 43 1964 5166 1739608
Pollakiuria 114.03 46.68 36 1971 2910 1741864
Bladder cancer 113.38 46.68 33 1974 2023 1742751
Acute kidney injury 89.56 46.68 65 1942 34879 1709895
Polyuria 81.00 46.68 23 1984 1287 1743487
Hyperglycaemia 80.08 46.68 32 1975 5133 1739641
Ketonuria 78.27 46.68 15 1992 140 1744634
Phimosis 72.26 46.68 14 1993 139 1744635
Diabetes mellitus inadequate control 69.11 46.68 22 1985 1820 1742954
Necrotising fasciitis 66.59 46.68 17 1990 632 1744142
Toe amputation 61.91 46.68 15 1992 448 1744326
Haematuria 59.20 46.68 29 1978 7531 1737243
Metabolic acidosis 58.69 46.68 26 1981 5376 1739398
Urosepsis 57.04 46.68 18 1989 1446 1743328
Thrombotic cerebral infarction 55.91 46.68 10 1997 61 1744713
Thirst 55.87 46.68 17 1990 1210 1743564
Acute myocardial infarction 52.85 46.68 28 1979 8559 1736215
Hypoglycaemia 47.68 46.68 26 1981 8412 1736362
Lactic acidosis 47.21 46.68 22 1985 5107 1739667

Pharmacologic Action:

SourceCodeDescription
ATC A10BD15 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD21 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD25 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BK01 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Sodium-glucose co-transporter 2 (SGLT2) inhibitors
CHEBI has role CHEBI:35526 hypoglycemic agent
FDA EPC N0000187059 Sodium-Glucose Cotransporter 2 Inhibitor
FDA MoA N0000187058 Sodium-Glucose Transporter 2 Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.62 acidic
pKa2 13.26 acidic
pKa3 13.7 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 6936590 Oct. 4, 2020 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO ARE ALREADY TREATED WITH DAPAGLIFLOZIN AND SAXAGLIPTIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 6936590 Oct. 4, 2020 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO HAVE INADEQUATE CONTROL WITH DAPAGLIFLOZIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 9198925 Oct. 4, 2020 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO ARE ALREADY TREATED WITH DAPAGLIFLOZIN AND SAXAGLIPTIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 9198925 Oct. 4, 2020 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO HAVE INADEQUATE CONTROL WITH DAPAGLIFLOZIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6414126 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 6936590 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 9198925 Oct. 4, 2020 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9238076 April 15, 2024 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9238076 April 15, 2024 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8431685 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8461105 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8431685 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8461105 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 7456254 June 30, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 7456254 June 30, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING FASTING PLASMA GLUCOSE IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING HBA1C IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8906851 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING FASTING PLASMA GLUCOSE IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING HBA1C IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8906851 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8501698 June 20, 2027 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO ARE ALREADY TREATED WITH DAPAGLIFLOZIN AND SAXAGLIPTIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8501698 June 20, 2027 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO HAVE INADEQUATE CONTROL WITH DAPAGLIFLOZIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8361972 March 21, 2028 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO ARE ALREADY TREATED WITH DAPAGLIFLOZIN AND SAXAGLIPTIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8361972 March 21, 2028 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO HAVE INADEQUATE CONTROL WITH DAPAGLIFLOZIN
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
10MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
2.5MG XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
5MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL Feb. 27, 2020 NEW COMBINATION
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Oct. 20, 2020 INFORMATION ADDED TO THE LABELING REGARDING THE SAFETY AND EFFICACY OF DAPAGLIFLOZIN IN PATIENTS WITH TYPE 2 DIABETES WHO HAVE INADEQUATE GLYCEMIC CONTROL ON A BACKGROUND COMBINATION OF METFORMIN AND EXENATIDE EXTENDED RELEASE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Oct. 20, 2020 INFORMATION ADDED TO THE LABELING REGARDING THE SAFETY AND EFFICACY OF DAPAGLIFLOZIN IN PATIENTS WITH TYPE 2 DIABETES WHO HAVE INADEQUATE GLYCEMIC CONTROL ON A BACKGROUND COMBINATION OF METFORMIN AND EXENATIDE EXTENDED RELEASE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Feb. 22, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO REFLECT THAT NO DOSE ADJUSTMENT IS NEEDED FOR PATIENTS WITH AN ESTIMATED GLOMERULAR FILTRATION RATE (EGFR) OF 45 ML/MIN/1.73 M2 OR GREATER AS SUPPORTED BY CLINICAL STUDY REPORT
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Feb. 22, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO REFLECT THAT NO DOSE ADJUSTMENT IS NEEDED FOR PATIENTS WITH AN ESTIMATED GLOMERULAR FILTRATION RATE (EGFR) OF 45 ML/MIN/1.73 M2 OR GREATER AS SUPPORTED BY CLINICAL STUDY REPORT
10MG QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL May 2, 2022 EXPANDED INDICATION FOR USE AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS
5MG QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL May 2, 2022 NEW STRENGTH
10MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT
2.5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT
5MG QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 RX TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium/glucose cotransporter 2 Transporter INHIBITOR IC50 9.30 IUPHAR IUPHAR
Low affinity sodium-glucose cotransporter Transporter IC50 8.87 CHEMBL
Sodium/glucose cotransporter 1 Transporter IC50 8.49 CHEMBL
Sodium/myo-inositol cotransporter 2 Transporter IC50 6.42 CHEMBL
Sodium/glucose cotransporter 2 Transporter EC50 8.52 CHEMBL

External reference:

IDSource
C3555622 UMLSCUI
D08897 KEGG_DRUG
1ULL0QJ8UC UNII
8886 INN_ID
703678003 SNOMEDCT_US
014949 NDDF
28989 MMSL
d07928 MMSL
1488564 RXNORM
4033035 VANDF
703674001 SNOMEDCT_US
960404-48-2 SECONDARY_CAS_RN
CHEMBL429910 ChEMBL_ID
DB06292 DRUGBANK_ID
CHEBI:85078 CHEBI
4594 IUPHAR_LIGAND_ID
CHEMBL2103802 ChEMBL_ID
9887712 PUBCHEM_CID
C529054 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 0310-6205 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 0310-6210 TABLET, FILM COATED 10 mg ORAL NDA 19 sections
XIGDUO HUMAN PRESCRIPTION DRUG LABEL 2 0310-6225 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL NDA 19 sections
XIGDUO HUMAN PRESCRIPTION DRUG LABEL 2 0310-6250 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 19 sections
XIGDUO HUMAN PRESCRIPTION DRUG LABEL 2 0310-6260 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 19 sections
XIGDUO HUMAN PRESCRIPTION DRUG LABEL 2 0310-6270 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 19 sections
XIGDUO HUMAN PRESCRIPTION DRUG LABEL 2 0310-6280 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 19 sections
QTERN HUMAN PRESCRIPTION DRUG LABEL 2 0310-6770 TABLET, FILM COATED 5 mg ORAL NDA 18 sections
QTERN HUMAN PRESCRIPTION DRUG LABEL 2 0310-6780 TABLET, FILM COATED 10 mg ORAL NDA 18 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 50090-3481 TABLET, FILM COATED 10 mg ORAL NDA 19 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 50090-3482 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 55154-6932 TABLET, FILM COATED 5 mg ORAL NDA 19 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 55154-6933 TABLET, FILM COATED 10 mg ORAL NDA 19 sections