saxagliptin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| dipeptidyl aminopeptidase-IV inhibitors | 4114 | 361442-04-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
inhibits Dipeptidyl Peptidase-4
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.23 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 63 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 24 % | Hosey CM, Chan R, Benet LZ |
| fu (Fraction unbound in plasma) | 1 % | Lombardo F, Berellini G, Obach RS |
| Vd (Volume of distribution) | 1.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 7.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 7.50 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 0.87 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 30, 2009 | EMA | ASTRAZENECA AB | |
| July 31, 2009 | FDA | ASTRAZENECA AB |
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 |
|---|---|---|---|---|---|---|
| Pancreatitis | 80.68 | 19.15 | 47 | 4291 | 49008 | 63435676 |
| Blood glucose increased | 51.64 | 19.15 | 44 | 4294 | 83712 | 63400972 |
| Ketoacidosis | 48.00 | 19.15 | 16 | 4322 | 4362 | 63480322 |
| Urinary tract obstruction | 36.35 | 19.15 | 11 | 4327 | 2197 | 63482487 |
| Hypoglycaemia | 35.87 | 19.15 | 31 | 4307 | 60034 | 63424650 |
| Acute lymphocytic leukaemia | 34.93 | 19.15 | 11 | 4327 | 2505 | 63482179 |
| Acute kidney injury | 32.91 | 19.15 | 62 | 4276 | 263353 | 63221331 |
| Lactic acidosis | 31.86 | 19.15 | 24 | 4314 | 38263 | 63446421 |
| Pancreatitis acute | 29.44 | 19.15 | 20 | 4318 | 27146 | 63457538 |
| Nausea | 29.07 | 19.15 | 125 | 4213 | 854346 | 62630338 |
| Dehydration | 28.39 | 19.15 | 46 | 4292 | 173308 | 63311376 |
| Diabetic ketoacidosis | 26.86 | 19.15 | 17 | 4321 | 20488 | 63464196 |
| Oedema peripheral | 26.67 | 19.15 | 47 | 4291 | 189464 | 63295220 |
| Arrhythmia | 25.47 | 19.15 | 21 | 4317 | 38119 | 63446565 |
| Abdominal pain | 23.82 | 19.15 | 58 | 4280 | 293398 | 63191286 |
| Inappropriate antidiuretic hormone secretion | 23.25 | 19.15 | 14 | 4324 | 15448 | 63469236 |
| Angioedema | 19.48 | 19.15 | 20 | 4318 | 47945 | 63436739 |
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 |
|---|---|---|---|---|---|---|
| Pancreatitis | 86.30 | 17.06 | 58 | 4712 | 38833 | 34913328 |
| Pancreatic carcinoma | 80.61 | 17.06 | 34 | 4736 | 8867 | 34943294 |
| Vertigo | 51.66 | 17.06 | 36 | 4734 | 25500 | 34926661 |
| Hypoglycaemia | 43.50 | 17.06 | 45 | 4725 | 54595 | 34897566 |
| Hypoglycaemic coma | 42.53 | 17.06 | 15 | 4755 | 2416 | 34949745 |
| Insulin C-peptide decreased | 41.41 | 17.06 | 7 | 4763 | 44 | 34952117 |
| Diabetic ketoacidotic hyperglycaemic coma | 39.46 | 17.06 | 8 | 4762 | 148 | 34952013 |
| Pancreatitis acute | 37.66 | 17.06 | 31 | 4739 | 28110 | 34924051 |
| Blood glucose increased | 36.15 | 17.06 | 45 | 4725 | 66673 | 34885488 |
| Dyspepsia | 32.41 | 17.06 | 32 | 4738 | 36700 | 34915461 |
| Dizziness | 32.09 | 17.06 | 83 | 4687 | 218438 | 34733723 |
| Diabetes mellitus inadequate control | 29.62 | 17.06 | 20 | 4750 | 13444 | 34938717 |
| Abdominal pain upper | 29.18 | 17.06 | 42 | 4728 | 71448 | 34880713 |
| Angina pectoris | 27.07 | 17.06 | 27 | 4743 | 31336 | 34920825 |
| Glycosylated haemoglobin increased | 25.29 | 17.06 | 17 | 4753 | 11343 | 34940818 |
| Volvulus | 24.52 | 17.06 | 9 | 4761 | 1623 | 34950538 |
| Acute kidney injury | 24.50 | 17.06 | 94 | 4676 | 304894 | 34647267 |
| Post procedural erythema | 23.70 | 17.06 | 3 | 4767 | 0 | 34952161 |
| Spleen congestion | 23.68 | 17.06 | 6 | 4764 | 309 | 34951852 |
| Medullary thyroid cancer | 22.01 | 17.06 | 4 | 4766 | 40 | 34952121 |
| Suprapubic pain | 21.49 | 17.06 | 6 | 4764 | 449 | 34951712 |
| Abnormal loss of weight | 19.43 | 17.06 | 10 | 4760 | 4080 | 34948081 |
| Ketoacidosis | 19.08 | 17.06 | 10 | 4760 | 4233 | 34947928 |
| Nausea | 19.02 | 17.06 | 94 | 4676 | 339814 | 34612347 |
| Renal disorder | 18.50 | 17.06 | 20 | 4750 | 25460 | 34926701 |
| Cardiac failure | 18.05 | 17.06 | 39 | 4731 | 91209 | 34860952 |
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 |
|---|---|---|---|---|---|---|
| Pancreatitis | 138.35 | 15.98 | 86 | 7928 | 68489 | 79667885 |
| Pancreatic carcinoma | 73.56 | 15.98 | 33 | 7981 | 13544 | 79722830 |
| Ketoacidosis | 65.69 | 15.98 | 26 | 7988 | 7828 | 79728546 |
| Pancreatitis acute | 63.55 | 15.98 | 47 | 7967 | 49557 | 79686817 |
| Blood glucose increased | 62.51 | 15.98 | 67 | 7947 | 114908 | 79621466 |
| Hypoglycaemia | 62.03 | 15.98 | 63 | 7951 | 101531 | 79634843 |
| Hypoglycaemic coma | 51.46 | 15.98 | 19 | 7995 | 4741 | 79731633 |
| Acute kidney injury | 50.81 | 15.98 | 140 | 7874 | 519264 | 79217110 |
| Insulin C-peptide decreased | 40.66 | 15.98 | 7 | 8007 | 70 | 79736304 |
| Diabetic ketoacidotic hyperglycaemic coma | 38.84 | 15.98 | 8 | 8006 | 221 | 79736153 |
| Lactic acidosis | 36.46 | 15.98 | 40 | 7974 | 70319 | 79666055 |
| Diabetes mellitus inadequate control | 35.66 | 15.98 | 25 | 7989 | 24239 | 79712135 |
| Dehydration | 32.67 | 15.98 | 75 | 7939 | 248112 | 79488262 |
| Diabetic ketoacidosis | 32.18 | 15.98 | 27 | 7987 | 34095 | 79702279 |
| Vertigo | 31.91 | 15.98 | 37 | 7977 | 69045 | 79667329 |
| Acute lymphocytic leukaemia | 29.88 | 15.98 | 13 | 8001 | 4956 | 79731418 |
| Angioedema | 29.06 | 15.98 | 37 | 7977 | 75998 | 79660376 |
| Cardiac failure | 28.84 | 15.98 | 54 | 7960 | 154788 | 79581586 |
| Angina pectoris | 27.82 | 15.98 | 30 | 7984 | 51702 | 79684672 |
| Nausea | 27.54 | 15.98 | 177 | 7837 | 957019 | 78779355 |
| Cerebral infarction | 27.26 | 15.98 | 28 | 7986 | 45648 | 79690726 |
| Dyspepsia | 26.91 | 15.98 | 43 | 7971 | 108644 | 79627730 |
| Glycosylated haemoglobin increased | 26.35 | 15.98 | 19 | 7995 | 19241 | 79717133 |
| Post procedural erythema | 24.62 | 15.98 | 3 | 8011 | 0 | 79736374 |
| Spleen congestion | 23.32 | 15.98 | 6 | 8008 | 448 | 79735926 |
| Pemphigoid | 23.01 | 15.98 | 16 | 7998 | 15299 | 79721075 |
| Volvulus | 22.49 | 15.98 | 9 | 8005 | 2787 | 79733587 |
| Arrhythmia | 22.13 | 15.98 | 29 | 7985 | 61243 | 79675131 |
| Urosepsis | 19.08 | 15.98 | 18 | 7996 | 26477 | 79709897 |
| Suprapubic pain | 18.69 | 15.98 | 6 | 8008 | 986 | 79735388 |
| Abdominal pain | 18.64 | 15.98 | 83 | 7931 | 389486 | 79346888 |
| Renal disorder | 18.52 | 15.98 | 22 | 7992 | 42083 | 79694291 |
| Urinary tract obstruction | 17.89 | 15.98 | 9 | 8005 | 4756 | 79731618 |
| Abdominal pain upper | 17.64 | 15.98 | 56 | 7958 | 223763 | 79512611 |
| Dizziness | 17.36 | 15.98 | 101 | 7913 | 526340 | 79210034 |
| Inappropriate antidiuretic hormone secretion | 17.29 | 15.98 | 17 | 7997 | 26296 | 79710078 |
| Weight decreased | 17.23 | 15.98 | 76 | 7938 | 355122 | 79381252 |
| Gamma-glutamyltransferase increased | 16.90 | 15.98 | 24 | 7990 | 54656 | 79681718 |
| Hyperglycaemia | 16.28 | 15.98 | 27 | 7987 | 70308 | 79666066 |
| Medullary thyroid cancer | 15.99 | 15.98 | 4 | 8010 | 267 | 79736107 |
| Pain | 15.98 | 15.98 | 29 | 7985 | 703773 | 79032601 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BD10 | 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 | A10BH03 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Dipeptidyl peptidase 4 (DPP-4) inhibitors |
| MeSH PA | D054873 | Dipeptidyl-Peptidase IV Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D006728 | Hormones |
| MeSH PA | D007004 | Hypoglycemic Agents |
| MeSH PA | D054795 | Incretins |
| MeSH PA | D011480 | Protease Inhibitors |
| CHEBI has role | CHEBI:35526 | antidiabetic |
| CHEBI has role | CHEBI:68612 | dipeptidyl peptidase-4 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 |
| Alcoholism | contraindication | 7200002 | |
| Asthenia | contraindication | 13791008 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Acute vomiting | contraindication | 23971007 | |
| Alcohol intoxication | contraindication | 25702006 | |
| Shock | contraindication | 27942005 | |
| Dehydration | contraindication | 34095006 | |
| Infectious disease | contraindication | 40733004 | |
| End stage renal disease | contraindication | 46177005 | DOID:784 |
| Lymphocytopenia | contraindication | 48813009 | DOID:614 |
| Ketoacidosis | contraindication | 56051008 | |
| Acute nephropathy | contraindication | 58574008 | |
| Metabolic acidosis | contraindication | 59455009 | |
| Hypopituitarism | contraindication | 74728003 | DOID:9406 |
| Cardiogenic shock | contraindication | 89138009 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Lactic acidosis | contraindication | 91273001 | DOID:3650 |
| Cobalamin deficiency | contraindication | 190634004 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Hypoglycemic disorder | contraindication | 237630007 | |
| Sepsis syndrome | contraindication | 238150007 | |
| Adrenal cortical hypofunction | contraindication | 386584007 | DOID:10493 |
| Fever | contraindication | 386661006 | |
| Surgical procedure | contraindication | 387713003 | |
| Severe diarrhea | contraindication | 409587002 | |
| Traumatic injury | contraindication | 417746004 | |
| Radiography with IV Iodinated Contrast Agent | contraindication | ||
| Severe Hypoxemia | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.77 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 2.5MG BASE | ONGLYZA | ASTRAZENECA AB | N022350 | July 31, 2009 | RX | TABLET | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES BY ADMINISTERING SAXAGLIPTIN |
| EQ 2.5MG BASE | ONGLYZA | ASTRAZENECA AB | N022350 | July 31, 2009 | RX | TABLET | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES MELLITUS BY ADMINISTERING SAXAGLIPTIN ALONE OR IN COMBINATION WITH INSULIN, METFORMIN, A THIAZOLIDINEDIONE, GLYBURIDE OR METFORMIN PLUS A SULFONYLUREA |
| EQ 5MG BASE | ONGLYZA | ASTRAZENECA AB | N022350 | July 31, 2009 | RX | TABLET | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES BY ADMINISTERING SAXAGLIPTIN |
| EQ 5MG BASE | ONGLYZA | ASTRAZENECA AB | N022350 | July 31, 2009 | RX | TABLET | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES MELLITUS BY ADMINISTERING SAXAGLIPTIN ALONE OR IN COMBINATION WITH INSULIN, METFORMIN, A THIAZOLIDINEDIONE, GLYBURIDE OR METFORMIN PLUS A SULFONYLUREA |
| 1GM;EQ 2.5MG BASE | KOMBIGLYZE XR | ASTRAZENECA AB | N200678 | Nov. 5, 2010 | RX | TABLET, EXTENDED RELEASE | ORAL | RE44186 | July 31, 2023 | ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS WHEN TREATMENT WITH BOTH SAXAGLIPTIN AND METFORMIN IS APPROPRIATE |
| 1GM;EQ 2.5MG BASE | KOMBIGLYZE XR | ASTRAZENECA AB | N200678 | Nov. 5, 2010 | RX | TABLET, EXTENDED RELEASE | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES MELLITUS BY ADMINISTERING SAXAGLIPTIN IN COMBINATION WITH METFORMIN |
| 1GM;EQ 5MG BASE | KOMBIGLYZE XR | ASTRAZENECA AB | N200678 | Nov. 5, 2010 | RX | TABLET, EXTENDED RELEASE | ORAL | RE44186 | July 31, 2023 | ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS WHEN TREATMENT WITH BOTH SAXAGLIPTIN AND METFORMIN IS APPROPRIATE |
| 1GM;EQ 5MG BASE | KOMBIGLYZE XR | ASTRAZENECA AB | N200678 | Nov. 5, 2010 | RX | TABLET, EXTENDED RELEASE | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES MELLITUS BY ADMINISTERING SAXAGLIPTIN IN COMBINATION WITH METFORMIN |
| 500MG;EQ 5MG BASE | KOMBIGLYZE XR | ASTRAZENECA AB | N200678 | Nov. 5, 2010 | RX | TABLET, EXTENDED RELEASE | ORAL | RE44186 | July 31, 2023 | ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS WHEN TREATMENT WITH BOTH SAXAGLIPTIN AND METFORMIN IS APPROPRIATE |
| 500MG;EQ 5MG BASE | KOMBIGLYZE XR | ASTRAZENECA AB | N200678 | Nov. 5, 2010 | RX | TABLET, EXTENDED RELEASE | ORAL | RE44186 | July 31, 2023 | METHOD FOR TREATING TYPE II DIABETES MELLITUS BY ADMINISTERING SAXAGLIPTIN IN COMBINATION WITH METFORMIN |
| 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;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;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;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 |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 2.5MG BASE | SAXAGLIPTIN | AMNEAL | A205941 | July 31, 2023 | RX | TABLET | ORAL | Jan. 27, 2024 | PATENT CHALLENGE |
| EQ 5MG BASE | SAXAGLIPTIN | AMNEAL | A205941 | July 31, 2023 | RX | TABLET | ORAL | Jan. 27, 2024 | PATENT CHALLENGE |
| EQ 2.5MG BASE | SAXAGLIPTIN | AUROBINDO PHARMA | A205972 | July 31, 2023 | RX | TABLET | ORAL | Jan. 27, 2024 | PATENT CHALLENGE |
| EQ 5MG BASE | SAXAGLIPTIN | AUROBINDO PHARMA | A205972 | July 31, 2023 | RX | TABLET | ORAL | Jan. 27, 2024 | PATENT CHALLENGE |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Dipeptidyl peptidase 4 | Enzyme | INHIBITOR | Ki | 9.22 | CHEMBL | CHEMBL | |||
| Cytochrome P450 3A4 | Enzyme | WOMBAT-PK | |||||||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| Dipeptidyl peptidase 8 | Enzyme | Ki | 6.89 | CHEMBL | |||||
| Dipeptidyl peptidase 9 | Enzyme | Ki | 7.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4029055 | VUID |
| N0000179814 | NUI |
| D08996 | KEGG_DRUG |
| 709031-78-7 | SECONDARY_CAS_RN |
| 4029055 | VANDF |
| 4029067 | VANDF |
| C1611934 | UMLSCUI |
| CHEBI:71272 | CHEBI |
| CHEMBL385517 | ChEMBL_ID |
| CHEMBL2103745 | ChEMBL_ID |
| CHEMBL1201743 | ChEMBL_ID |
| DB06335 | DRUGBANK_ID |
| C502994 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11243969 | PUBCHEM_CID |
| 6316 | IUPHAR_LIGAND_ID |
| 9GB927LAJW | UNII |
| 1043560 | RXNORM |
| 166611 | MMSL |
| 26648 | MMSL |
| 32427 | MMSL |
| 369212 | MMSL |
| d07467 | MMSL |
| 013204 | NDDF |
| 013205 | NDDF |
| 443066009 | SNOMEDCT_US |
| 443087004 | SNOMEDCT_US |
| 734452007 | SNOMEDCT_US |
| BJM | PDB_CHEM_ID |
| 945667-22-1 | SECONDARY_CAS_RN |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ONGLYZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-6100 | TABLET, FILM COATED | 2.50 mg | ORAL | NDA | 30 sections |
| ONGLYZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-6105 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 30 sections |
| KOMBIGLYZEXR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6125 | TABLET, FILM COATED, EXTENDED RELEASE | 2.50 mg | ORAL | NDA | 30 sections |
| KOMBIGLYZEXR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6125 | TABLET, FILM COATED, EXTENDED RELEASE | 2.50 mg | ORAL | NDA | 30 sections |
| KOMBIGLYZEXR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6135 | TABLET, FILM COATED, EXTENDED RELEASE | 5 mg | ORAL | NDA | 30 sections |
| KOMBIGLYZEXR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6135 | TABLET, FILM COATED, EXTENDED RELEASE | 5 mg | ORAL | NDA | 30 sections |
| KOMBIGLYZEXR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6145 | TABLET, FILM COATED, EXTENDED RELEASE | 5 mg | ORAL | NDA | 30 sections |
| KOMBIGLYZEXR | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6145 | TABLET, FILM COATED, EXTENDED RELEASE | 5 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 | 0310-6770 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 28 sections |
| QTERN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6780 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 28 sections |
| QTERN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6780 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 28 sections |
| QTERN | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0310-6780 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 28 sections |
| Saxagliptin and Metformin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43598-618 | TABLET, FILM COATED, EXTENDED RELEASE | 2.50 mg | ORAL | ANDA | 27 sections |
| Saxagliptin and Metformin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43598-619 | TABLET, FILM COATED, EXTENDED RELEASE | 5 mg | ORAL | ANDA | 27 sections |
| Saxagliptin and Metformin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 2 | 43598-620 | TABLET, FILM COATED, EXTENDED RELEASE | 5 mg | ORAL | ANDA | 27 sections |
| ONGLYZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6309 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 31 sections |
| ONGLYZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55154-6931 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 30 sections |
| ONGLYZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55154-6931 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 30 sections |
| Saxagliptin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-059 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 23 sections |
| Saxagliptin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-060 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 23 sections |
| Saxagliptin | Human Prescription Drug Label | 1 | 65862-825 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 27 sections |
| Saxagliptin | Human Prescription Drug Label | 1 | 65862-826 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 27 sections |
| SAXAGLIPTIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-726 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 28 sections |
| SAXAGLIPTIN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-727 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 28 sections |