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

Stem definition	Drug id	CAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives	4304	461432-26-8

Description:

Molecule	Description
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: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company
March 24, 2014	PMDA	BRISTOL-MYERS
Jan. 8, 2014	FDA	ASTRAZENECA AB
Nov. 12, 2012	EMA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Diabetic ketoacidosis	3100.88	18.82	719	9724	17153	50577528
Ketoacidosis	1369.35	18.82	281	10162	3614	50591067
Euglycaemic diabetic ketoacidosis	935.45	18.82	194	10249	2625	50592056
Fungal infection	354.82	18.82	156	10287	29809	50564872
Ketosis	179.15	18.82	37	10406	486	50594195
Diabetes mellitus inadequate control	147.56	18.82	66	10377	13079	50581602
Glycosylated haemoglobin increased	137.70	18.82	59	10384	10547	50584134
Ketonuria	130.65	18.82	28	10415	444	50594237
Urinary tract infection	127.21	18.82	191	10252	223829	50370852
Blood glucose increased	102.85	18.82	98	10345	71226	50523455
Hypoglycaemia	91.59	18.82	81	10362	53500	50541181
Lactic acidosis	90.25	18.82	66	10377	33289	50561392
Blood ketone body increased	86.07	18.82	18	10425	252	50594429
Diabetic metabolic decompensation	81.07	18.82	24	10419	1456	50593225
Acute kidney injury	76.18	18.82	154	10289	227904	50366777
Glomerular filtration rate decreased	74.93	18.82	40	10403	11612	50583069
Urine ketone body present	74.26	18.82	25	10418	2308	50592373
Weight decreased	71.04	18.82	147	10296	221098	50373583
Dehydration	69.81	18.82	118	10325	152331	50442350
Metabolic acidosis	68.95	18.82	60	10383	38765	50555916
Diabetic ketosis	68.12	18.82	14	10429	179	50594502
Hyperglycaemia	58.16	18.82	53	10390	36352	50558329
Vulvovaginal pruritus	53.72	18.82	20	10423	2476	50592205
Pyelonephritis	53.06	18.82	35	10408	14954	50579727
Necrotising fasciitis	52.89	18.82	20	10423	2584	50592097
Genital infection female	51.76	18.82	10	10433	91	50594590
Pruritus genital	51.74	18.82	14	10429	612	50594069
Temperature perception test abnormal	50.78	18.82	8	10435	17	50594664
Glucose urine present	45.83	18.82	13	10430	677	50594004
Left ventricular dysfunction	43.29	18.82	27	10416	10479	50584202
Candida infection	43.05	18.82	37	10406	23486	50571195
Pollakiuria	40.60	18.82	36	10407	23815	50570866
Urosepsis	40.45	18.82	30	10413	15435	50579246
Cerebral infarction	39.58	18.82	34	10409	21570	50573111
Polyuria	39.02	18.82	22	10421	7099	50587582
Genital infection	37.61	18.82	7	10436	51	50594630
Genital infection fungal	34.98	18.82	8	10435	173	50594508
Decreased vibratory sense	32.60	18.82	8	10435	236	50594445
Drug ineffective	31.93	18.82	77	10366	819256	49775425
Acidosis	31.70	18.82	22	10421	10205	50584476
Bladder trabeculation	31.11	18.82	6	10437	54	50594627
Haematuria	30.94	18.82	32	10411	25581	50569100
Pancreatitis	29.43	18.82	40	10403	42574	50552107
Cardiac failure	28.50	18.82	54	10389	75986	50518695
Vulvovaginal mycotic infection	27.58	18.82	15	10428	4514	50590167
Blood glucose abnormal	27.12	18.82	17	10426	6655	50588026
Dysuria	26.44	18.82	31	10412	28473	50566208
Peripartum cardiomyopathy	26.22	18.82	6	10437	130	50594551
Toe amputation	26.20	18.82	11	10432	1866	50592815
Urinary tract infection fungal	25.69	18.82	8	10435	576	50594105
Compartment syndrome	25.63	18.82	11	10432	1971	50592710
Blood ketone body	25.54	18.82	5	10438	49	50594632
Suspected COVID-19	25.32	18.82	10	10433	1451	50593230
Pain	25.28	18.82	51	10392	578852	50015829
Hyperglycaemic hyperosmolar nonketotic syndrome	25.22	18.82	8	10435	612	50594069
Vomiting	24.72	18.82	171	10272	460587	50134094
Arteriosclerosis	24.62	18.82	18	10425	9059	50585622
Capillary leak syndrome	22.84	18.82	10	10433	1880	50592801
Dizziness	22.52	18.82	135	10308	346234	50248447
Perineal pain	22.43	18.82	6	10437	251	50594430
Latent autoimmune diabetes in adults	22.31	18.82	4	10439	23	50594658
Portal fibrosis	22.13	18.82	6	10437	264	50594417
Thirst	22.06	18.82	18	10425	10632	50584049
Upper airway obstruction	21.69	18.82	7	10436	566	50594115
Food refusal	21.09	18.82	6	10437	316	50594365
Atrioventricular block complete	21.07	18.82	15	10428	7240	50587441
Contraindicated product administered	20.80	18.82	3	10440	148955	50445726
Glycosuria	20.77	18.82	8	10435	1086	50593595
Pyelonephritis acute	20.72	18.82	12	10431	4071	50590610
Toxicity to various agents	20.66	18.82	9	10434	212490	50382191
Rheumatoid arthritis	20.63	18.82	8	10435	202542	50392139
Aortic valve calcification	19.70	18.82	6	10437	401	50594280
Vulvovaginal candidiasis	19.46	18.82	10	10433	2682	50591999
Orthopnoea	19.44	18.82	13	10430	5676	50589005
Diabetic ketoacidotic hyperglycaemic coma	19.33	18.82	4	10439	53	50594628
Metabolic alkalosis	19.33	18.82	10	10433	2721	50591960
Hyperkalaemia	19.07	18.82	35	10408	48054	50546627

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Diabetic ketoacidosis	2177.06	17.82	601	10676	15472	29547778
Ketoacidosis	782.36	17.82	197	11080	3442	29559808
Euglycaemic diabetic ketoacidosis	618.26	17.82	153	11124	2477	29560773
Glycosylated haemoglobin increased	207.00	17.82	91	11186	9335	29553915
Ketosis	175.26	17.82	39	11238	384	29562866
Ketonuria	147.60	17.82	36	11241	544	29562706
Phimosis	136.64	17.82	35	11242	652	29562598
Balanoposthitis	128.08	17.82	36	11241	966	29562284
Blood glucose increased	107.22	17.82	122	11155	58862	29504388
Fungal infection	104.32	17.82	65	11212	13620	29549630
Diabetic ketosis	99.26	17.82	19	11258	80	29563170
Glomerular filtration rate abnormal	91.78	17.82	26	11251	718	29562532
Metabolic acidosis	89.79	17.82	90	11187	37572	29525678
Glomerular filtration rate decreased	89.64	17.82	55	11222	11211	29552039
Lactic acidosis	88.63	17.82	81	11196	30166	29533084
Diabetes mellitus inadequate control	88.38	17.82	56	11221	12078	29551172
Polyuria	82.74	17.82	45	11232	7317	29555933
N-terminal prohormone brain natriuretic peptide increased	81.98	17.82	30	11247	1902	29561348
Toe amputation	78.79	17.82	30	11247	2125	29561125
Hypoglycaemia	74.57	17.82	92	11185	48254	29514996
Bladder cancer	74.40	17.82	47	11230	10080	29553170
Weight decreased	73.36	17.82	171	11106	150734	29412516
Blood ketone body increased	68.86	17.82	18	11259	364	29562886
Urinary tract infection	67.27	17.82	108	11169	72246	29491004
Type V hyperlipidaemia	66.70	17.82	20	11257	677	29562573
Necrotising fasciitis	65.88	17.82	30	11247	3335	29559915
Pollakiuria	65.17	17.82	53	11224	16863	29546387
Dehydration	61.23	17.82	135	11142	114613	29448637
Epididymitis	60.57	17.82	25	11252	2190	29561060
Acquired phimosis	60.19	17.82	12	11265	65	29563185
Urine ketone body present	54.79	17.82	19	11258	1029	29562221
Blood pressure decreased	52.32	17.82	75	11202	45402	29517848
Cerebral infarction	49.85	17.82	54	11223	24621	29538629
Hyperglycaemia	47.68	17.82	62	11215	34225	29529025
Glucose urine present	44.61	17.82	16	11261	957	29562293
Urosepsis	44.21	17.82	35	11242	10711	29552539
Hyperglycaemic hyperosmolar nonketotic syndrome	43.12	17.82	16	11261	1054	29562196
Cardiac failure	43.05	17.82	94	11183	79193	29484057
Acute kidney injury	42.17	17.82	206	11071	265061	29298189
Thirst	40.02	17.82	27	11250	6464	29556786
Mitral valve thickening	36.98	17.82	11	11266	362	29562888
Toxicity to various agents	35.61	17.82	11	11266	173650	29389600
Glycosuria	34.79	17.82	14	11263	1148	29562102
Thrombotic cerebral infarction	34.07	17.82	10	11267	314	29562936
Mitral valve calcification	33.05	17.82	11	11266	525	29562725
Ejection fraction decreased	32.32	17.82	35	11242	15943	29547307
Neutropenia	31.56	17.82	6	11271	131705	29431545
Blood glucose abnormal	30.99	17.82	21	11256	5062	29558188
Thrombocytopenia	30.54	17.82	7	11270	134816	29428434
Genital rash	30.34	17.82	10	11267	463	29562787
N-terminal prohormone brain natriuretic peptide abnormal	29.34	17.82	8	11269	191	29563059
Foot amputation	29.33	17.82	10	11267	514	29562736
Acute myocardial infarction	29.24	17.82	60	11217	48378	29514872
Perineal abscess	28.55	17.82	8	11269	212	29563038
Body mass index increased	28.33	17.82	11	11266	821	29562429
Gangrene	27.09	17.82	18	11259	4200	29559050
Microalbuminuria	26.96	17.82	10	11267	658	29562592
Obesity	26.14	17.82	25	11252	9838	29553412
Total cholesterol/HDL ratio increased	25.80	17.82	7	11270	164	29563086
Genital infection fungal	25.60	17.82	7	11270	169	29563081
Febrile neutropenia	25.07	17.82	6	11271	112234	29451016
Mitral valve incompetence	24.95	17.82	28	11249	13265	29549985
Pancreatitis	24.77	17.82	46	11231	34468	29528782
Cardiac failure chronic	24.34	17.82	20	11257	6447	29556803
Pancreatitis acute	23.43	17.82	37	11240	24348	29538902
Hyperuricaemia	23.24	17.82	20	11257	6869	29556381
Hypertrophy	22.89	17.82	8	11269	443	29562807
Genital infection male	22.78	17.82	4	11273	9	29563241
Peripheral circulatory failure	22.47	17.82	6	11271	132	29563118
Urine output increased	22.44	17.82	10	11267	1056	29562194
Renal atrophy	22.25	17.82	10	11267	1077	29562173
Acetonaemia	22.10	17.82	6	11271	141	29563109
Immune-mediated hepatitis	21.91	17.82	11	11266	1516	29561734
Brain stem infarction	21.88	17.82	10	11267	1120	29562130
Vaccination failure	21.69	17.82	8	11269	518	29562732
Bladder cancer recurrent	21.43	17.82	7	11270	315	29562935
Diabetes mellitus	21.33	17.82	47	11230	39784	29523466
Haematuria	21.32	17.82	50	11227	44089	29519161
Disease progression	21.24	17.82	3	11274	81913	29481337
Hypoglycaemic coma	20.96	17.82	12	11265	2151	29561099
Polycythaemia	20.53	17.82	11	11266	1733	29561517
Drug ineffective	20.25	17.82	71	11206	363099	29200151
Type 2 diabetes mellitus	19.56	17.82	25	11252	13556	29549694
Pancytopenia	19.47	17.82	4	11273	83164	29480086
Pyrexia	19.02	17.82	52	11225	287570	29275680
Pyelonephritis	18.89	17.82	16	11261	5377	29557873
Dysuria	18.79	17.82	32	11245	22408	29540842
Anaemia	18.59	17.82	30	11247	200921	29362329
Malignant neoplasm progression	18.47	17.82	3	11274	73856	29489394
Concomitant disease aggravated	17.91	17.82	15	11262	4963	29558287

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Diabetic ketoacidosis	4112.57	16.15	1065	17416	28780	64451471
Ketoacidosis	1605.04	16.15	376	18105	6487	64473764
Euglycaemic diabetic ketoacidosis	1352.55	16.15	313	18168	5097	64475154
Ketosis	291.10	16.15	65	18416	888	64479363
Glycosylated haemoglobin increased	253.91	16.15	113	18368	15906	64464345
Ketonuria	223.32	16.15	54	18427	1063	64479188
Diabetes mellitus inadequate control	205.73	16.15	107	18374	21214	64459037
Lactic acidosis	166.28	16.15	139	18342	61271	64418980
Metabolic acidosis	160.61	16.15	145	18336	70813	64409438
Hypoglycaemia	151.20	16.15	156	18325	89736	64390515
Diabetic ketosis	145.74	16.15	31	18450	332	64479919
Fungal infection	142.17	16.15	100	18381	34151	64446100
Blood glucose increased	138.22	16.15	155	18326	97918	64382333
Dehydration	119.76	16.15	219	18262	216544	64263707
Acute kidney injury	115.31	16.15	335	18146	448905	64031346
Glomerular filtration rate decreased	112.42	16.15	70	18411	19502	64460749
Cerebral infarction	105.08	16.15	90	18391	40954	64439297
Polyuria	103.78	16.15	57	18424	12586	64467665
Hyperglycaemia	102.80	16.15	106	18375	60862	64419389
Weight decreased	99.58	16.15	239	18242	285500	64194751
Urine ketone body present	99.58	16.15	37	18444	3270	64476981
Blood ketone body increased	98.39	16.15	25	18456	607	64479644
Balanoposthitis	97.13	16.15	26	18455	778	64479473
Urinary tract infection	96.54	16.15	208	18273	231388	64248863
Toe amputation	93.94	16.15	36	18445	3464	64476787
Necrotising fasciitis	92.21	16.15	40	18441	5286	64474965
Glomerular filtration rate abnormal	85.60	16.15	26	18455	1233	64479018
Glucose urine present	78.96	16.15	26	18455	1606	64478645
Pollakiuria	78.39	16.15	68	18413	31462	64448789
Diabetic metabolic decompensation	73.00	16.15	28	18453	2700	64477551
Phimosis	71.81	16.15	18	18463	413	64479838
Type V hyperlipidaemia	71.16	16.15	21	18460	901	64479350
N-terminal prohormone brain natriuretic peptide increased	69.13	16.15	29	18452	3530	64476721
Cardiac failure	65.84	16.15	128	18353	132245	64348006
Hyperglycaemic hyperosmolar nonketotic syndrome	62.09	16.15	22	18459	1697	64478554
Epididymitis	61.65	16.15	22	18459	1732	64478519
Urosepsis	57.65	16.15	49	18432	22045	64458206
Pyelonephritis	54.97	16.15	43	18438	17223	64463028
Pruritus genital	52.18	16.15	17	18464	1015	64479236
Toxicity to various agents	51.35	16.15	20	18461	363493	64116758
Thrombotic cerebral infarction	50.81	16.15	14	18467	468	64479783
Temperature perception test abnormal	48.16	16.15	8	18473	17	64480234
Bladder cancer	47.75	16.15	33	18448	10941	64469310
Drug ineffective	46.66	16.15	108	18373	840139	63640112
Genital infection female	45.60	16.15	9	18472	64	64480187
Blood pressure decreased	44.85	16.15	85	18396	86114	64394137
Thirst	44.55	16.15	35	18446	14102	64466149
Blood glucose abnormal	44.03	16.15	29	18452	8884	64471367
Left ventricular dysfunction	43.01	16.15	37	18444	16917	64463334
Acute myocardial infarction	42.96	16.15	74	18407	69644	64410607
Acquired phimosis	42.62	16.15	8	18473	42	64480209
Haematuria	42.37	16.15	68	18413	60403	64419848
Vulvovaginal pruritus	42.18	16.15	17	18464	1869	64478382
Genital infection	41.16	16.15	8	18473	52	64480199
Dysuria	40.60	16.15	55	18426	42002	64438249
Mitral valve thickening	39.30	16.15	11	18470	390	64479861
Acetonaemia	38.59	16.15	10	18471	263	64479988
Pancreatitis acute	38.30	16.15	54	18427	42801	64437450
Congenital hydrocephalus	37.92	16.15	7	18474	33	64480218
Suspected COVID-19	37.63	16.15	15	18466	1602	64478649
Glycosuria	37.29	16.15	16	18465	2058	64478193
Hypoglycaemic coma	37.10	16.15	20	18461	4254	64475997
Body mass index increased	34.51	16.15	14	18467	1565	64478686
Infusion related reaction	33.31	16.15	4	18477	164463	64315788
Pancreatitis	32.52	16.15	60	18421	59547	64420704
Neutropenia	32.48	16.15	14	18467	239610	64240641
N-terminal prohormone brain natriuretic peptide abnormal	29.67	16.15	8	18473	246	64480005
Pancreatic carcinoma	29.11	16.15	24	18457	10349	64469902
Perineal abscess	28.96	16.15	9	18472	461	64479790
Bladder trabeculation	28.76	16.15	6	18475	58	64480193
Mitral valve incompetence	28.70	16.15	36	18445	25502	64454749
Joint swelling	28.53	16.15	13	18468	215369	64264882
Microalbuminuria	27.23	16.15	10	18471	855	64479396
Brain stem infarction	26.14	16.15	12	18469	1811	64478440
Thrombocytopenia	25.98	16.15	16	18465	223785	64256466
Total cholesterol/HDL ratio increased	25.88	16.15	7	18474	218	64480033
Mitral valve calcification	25.86	16.15	11	18470	1385	64478866
Hypersensitivity	25.80	16.15	12	18469	196440	64283811
Diabetes mellitus	25.67	16.15	58	18423	66416	64413835
Disease progression	25.16	16.15	5	18476	141675	64338576
Drug abuse	24.96	16.15	4	18477	132370	64347881
Acidosis	24.80	16.15	28	18453	17767	64462484
Obesity	24.74	16.15	30	18451	20532	64459719
Peripartum cardiomyopathy	24.48	16.15	6	18475	125	64480126
Vomiting	24.41	16.15	253	18228	550864	63929387
Arthropathy	24.35	16.15	3	18478	120964	64359287
Shock	24.09	16.15	41	18440	38199	64442052
White blood cell count decreased	23.41	16.15	8	18473	157829	64322422
Hyperuricaemia	23.36	16.15	21	18460	10170	64470081
Pain	23.34	16.15	81	18400	553430	63926821
Treatment failure	23.26	16.15	3	18478	116813	64363438
Decreased vibratory sense	22.97	16.15	8	18473	586	64479665
Genital infection fungal	22.83	16.15	6	18475	167	64480084
Gangrene	22.76	16.15	18	18463	7320	64472931
Musculoskeletal stiffness	22.62	16.15	4	18477	123202	64357049
Immune-mediated hepatitis	22.59	16.15	12	18469	2477	64477774
Hyperkalaemia	22.56	16.15	72	18409	101057	64379194
Perineal pain	22.29	16.15	9	18472	994	64479257
Low density lipoprotein increased	21.91	16.15	18	18463	7722	64472529
Foot amputation	21.68	16.15	8	18473	693	64479558
Cardiac failure chronic	21.46	16.15	19	18462	9022	64471229
Urinary retention	21.35	16.15	45	18436	49156	64431095
Condition aggravated	21.27	16.15	47	18434	372379	64107872
Ejection fraction decreased	21.09	16.15	33	18448	28674	64451577
Hypertrophy	21.05	16.15	8	18473	752	64479499
Renal atrophy	20.91	16.15	10	18471	1654	64478597
Pyrexia	20.79	16.15	86	18395	558558	63921693
Hypernatraemia	20.17	16.15	21	18460	12168	64468083
High density lipoprotein decreased	19.88	16.15	13	18468	3933	64476318
Vaccination failure	19.82	16.15	8	18473	883	64479368
Urinary tract infection fungal	19.78	16.15	8	18473	887	64479364
COVID-19 pneumonia	19.72	16.15	24	18457	16480	64463771
Polydipsia	19.62	16.15	15	18466	5806	64474445
Polycythaemia	19.23	16.15	10	18471	1977	64478274
Renal impairment	19.10	16.15	83	18398	134934	64345317
Vulvovaginal candidiasis	18.58	16.15	10	18471	2120	64478131
Diabetic retinopathy	18.46	16.15	11	18470	2828	64477423
Pancytopenia	18.43	16.15	9	18472	143300	64336951
Febrile neutropenia	18.42	16.15	16	18465	187641	64292610
Heat illness	18.12	16.15	6	18475	377	64479874
Malignant neoplasm progression	18.03	16.15	5	18476	112866	64367385
Coronary artery stenosis	17.94	16.15	19	18462	11229	64469022
Bladder transitional cell carcinoma	17.74	16.15	10	18471	2320	64477931
Urine ketone body	17.60	16.15	5	18476	187	64480064
Depression	17.54	16.15	16	18465	183275	64296976
Food refusal	17.11	16.15	6	18475	449	64479802
Urine output increased	16.97	16.15	9	18472	1852	64478399
Aortic valve incompetence	16.88	16.15	16	18465	8285	64471966
Insulin C-peptide decreased	16.88	16.15	4	18477	72	64480179
Diabetic ketoacidotic hyperglycaemic coma	16.82	16.15	5	18476	220	64480031
Contraindicated product administered	16.81	16.15	5	18476	107824	64372427
Pneumonia	16.81	16.15	93	18388	559483	63920768
Pyelonephritis acute	16.80	16.15	13	18468	5121	64475130
Abnormal loss of weight	16.47	16.15	15	18466	7385	64472866
Candida infection	16.35	16.15	31	18450	31388	64448863

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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
MeSH PA	D007004	Hypoglycemic Agents
MeSH PA	D000077203	Sodium-Glucose Transporter 2 Inhibitors
FDA MoA	N0000187058	Sodium-Glucose Transporter 2 Inhibitors
FDA EPC	N0000187059	Sodium-Glucose Cotransporter 2 Inhibitor
CHEBI has role	CHEBI:35526	antidiabetic
CHEBI has role	CHEBI:73273	sodium-glucose transport protein subtype 2 inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Diabetes mellitus type 2	indication	44054006	DOID:9352
Diabetes mellitus type 1	indication	46635009	DOID:9744
Chronic heart failure	indication	48447003
Chronic kidney disease	indication	709044004

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.62	acidic
pKa2	13.26	acidic
pKa3	13.7	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	Feb. 27, 2017	RX	TABLET	ORAL	RE44186	July 31, 2023	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	May 2, 2019	RX	TABLET	ORAL	RE44186	July 31, 2023	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	RE44186	July 31, 2023	TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	RE44186	July 31, 2023	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	RE44186	July 31, 2023	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	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	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;500MG	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	July 28, 2017	RX	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;500MG	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	Feb. 27, 2017	RX	TABLET	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	May 2, 2019	RX	TABLET	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	6515117	Oct. 4, 2025	TREATMENT OF TYPE 2 DIABETES MELLITUS
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;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;500MG	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;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	July 28, 2017	RX	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;500MG	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;EQ 5MG BASE	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;EQ 5MG BASE	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;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	Feb. 27, 2017	RX	TABLET	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	May 2, 2019	RX	TABLET	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	8501698	June 20, 2027	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	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;EQ 5MG BASE	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;EQ 5MG BASE	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;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	Feb. 27, 2017	RX	TABLET	ORAL	8361972	March 21, 2028	TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE	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;1GM	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
10MG;500MG	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;1GM	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;1GM	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
5MG;500MG	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
10MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	10973836	March 9, 2040	REDUCTION OF THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH HEART FAILURE WITH REDUCED EJECTION FRACTION AND WITHOUT TYPE II DIABETES

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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;EQ 5MG BASE	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;EQ 5MG BASE	QTERN	ASTRAZENECA AB	N209091	May 2, 2019	RX	TABLET	ORAL	May 2, 2022	NEW STRENGTH
10MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	May 2, 2022	NEW PRODUCT
2.5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	May 2, 2022	NEW PRODUCT
5MG;1GM;EQ 2.5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	May 2, 2022	NEW PRODUCT
5MG;1GM;EQ 5MG BASE	QTERNMET XR	ASTRAZENECA AB	N210874	May 2, 2019	DISCN	TABLET, EXTENDED RELEASE	ORAL	May 2, 2022	NEW PRODUCT
10MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
5MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
10MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
10MG;500MG	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
2.5MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	July 28, 2017	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
5MG;1GM	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
5MG;500MG	XIGDUO XR	ASTRAZENECA AB	N205649	Oct. 29, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2022	TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
10MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	May 5, 2023	TO REDUCE THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH HEART FAILURE (NYHA CLASS II-IV) WITH REDUCED EJECTION FRACTION
5MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	May 5, 2023	TO REDUCE THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH HEART FAILURE (NYHA CLASS II-IV) WITH REDUCED EJECTION FRACTION
10MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	April 30, 2024	TO REDUCE THE RISK OF SUSTAINED EGFR DECLINE, END-STAGE KIDNEY DISEASE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH CHRONIC KIDNEY DISEASE AT RISK OF PROGRESSION
5MG	FARXIGA	ASTRAZENECA AB	N202293	Jan. 8, 2014	RX	TABLET	ORAL	April 30, 2024	TO REDUCE THE RISK OF SUSTAINED EGFR DECLINE, END-STAGE KIDNEY DISEASE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH CHRONIC KIDNEY DISEASE AT RISK OF PROGRESSION

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium/glucose cotransporter 2	Transporter	P31639	SC5A2_HUMAN	INHIBITOR	IC50	9.30	IUPHAR	IUPHAR
Sodium/glucose cotransporter 1	Transporter	P13866	SC5A1_HUMAN		IC50	8.49	CHEMBL
Sodium/myo-inositol cotransporter 2	Transporter	Q8WWX8	SC5AB_HUMAN		IC50	6.42	CHEMBL
Low affinity sodium-glucose cotransporter	Transporter	Q9NY91	SC5A4_HUMAN		IC50	8.87	CHEMBL
Sodium/glucose cotransporter 2	Transporter		SC5A2_RAT		EC50	8.52	CHEMBL

External reference:

ID	Source
D08897	KEGG_DRUG
960404-48-2	SECONDARY_CAS_RN
4033035	VANDF
CHEBI:85078	CHEBI
CHEMBL429910	ChEMBL_ID
CHEMBL2103802	ChEMBL_ID
C529054	MESH_SUPPLEMENTAL_RECORD_UI
4594	IUPHAR_LIGAND_ID
8886	INN_ID
DB06292	DRUGBANK_ID
1ULL0QJ8UC	UNII
9887712	PUBCHEM_CID
1486966	RXNORM
210769	MMSL
28989	MMSL
29986	MMSL
d07928	MMSL
014949	NDDF
014950	NDDF
703674001	SNOMEDCT_US
703675000	SNOMEDCT_US
703678003	SNOMEDCT_US
783086004	SNOMEDCT_US
C2353951	UMLSCUI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	0310-6205	TABLET, FILM COATED	5 mg	ORAL	NDA	27 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	0310-6210	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6225	TABLET, FILM COATED, EXTENDED RELEASE	2.50 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6225	TABLET, FILM COATED, EXTENDED RELEASE	2.50 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6250	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6250	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6260	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6260	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6270	TABLET, FILM COATED, EXTENDED RELEASE	10 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6270	TABLET, FILM COATED, EXTENDED RELEASE	10 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6280	TABLET, FILM COATED, EXTENDED RELEASE	10 mg	ORAL	NDA	30 sections
XIGDUOXR	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6280	TABLET, FILM COATED, EXTENDED RELEASE	10 mg	ORAL	NDA	30 sections
QTERN	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6770	TABLET, FILM COATED	5 mg	ORAL	NDA	28 sections
QTERN	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6770	TABLET, FILM COATED	5 mg	ORAL	NDA	28 sections
QTERN	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6780	TABLET, FILM COATED	10 mg	ORAL	NDA	28 sections
QTERN	HUMAN PRESCRIPTION DRUG LABEL	2	0310-6780	TABLET, FILM COATED	10 mg	ORAL	NDA	28 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3481	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3482	TABLET, FILM COATED	5 mg	ORAL	NDA	27 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-6932	TABLET, FILM COATED	5 mg	ORAL	NDA	27 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-6932	TABLET, FILM COATED	5 mg	ORAL	NDA	27 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-6933	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections
FARXIGA	HUMAN PRESCRIPTION DRUG LABEL	1	55154-6933	TABLET, FILM COATED	10 mg	ORAL	NDA	27 sections