Repaglinide
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1997
- First approval year
- 1997
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Repaglinide
- Molecular weight
- 452.6
- Structure (SMILES)
- CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O
- enyglid
- Enyglid
- novonorm
- Novonorm
- prandin
- Prandin
- repaglinide
- Repaglinide
- repaglinide accord
- Repaglinide accord
- repaglinide component of prandimet
- Repaglinide component of prandimet
- repaglinide krka
- Repaglinide krka
- repaglinide teva
- Repaglinide teva
- (+)-2-ETHOXY-.ALPHA.-(((S)-.ALPHA.-ISOBUTYL-O-PIPERIDINOBENZYL)CARBAMOYL)-P-TOLUIC ACID
- 2 ethoxy alpha s alpha isobutyl o piperidinobenzyl carbamoyl p toluic acid
- a10bx02
- A10BX02
- ag ee 388 zw
- ag ee 623 zw
- ag ee 623zw
- AG-EE 388 ZW
- AG-EE 623 ZW
- AG-EE 623ZW
- AG-EE-623-ZW
- AG-EE-623ZW
- agee 623zw
- AGEE-623ZW
- chembl1272
- CHEMBL1272
- enyglid
- ENYGLID
- novonorm
- NOVONORM
- nsc 759893
- NSC-759893
- prandin
- PRANDIN
- repaglinida
And 40 more, listed on the interactive page.
- ATC classification codes
- A10BX02
Sources for recorded values
- CAS registry numbers
- 135062-02-1
- ChEMBL ID
- CHEMBL1272
- InChIKey
- FAEKWTJYAYMJKF-QHCPKHFHSA-N
- PubChem compound IDs
- 65981
- RxNorm IDs (RxCUI)
- 73044
- FDA ingredient codes (UNII)
- 668Z8C33LU
- Applicant
- GEMINI LABS LLC
- Approval date
- 22 Dec 1997
- Application number
- NDA020741
- Status
- Authorised
- Status date
- 16 Aug 1998
- Authorisation date
- 16 Aug 1998
- Approved indications
- Repaglinide is indicated in patients with type-2 diabetes (non-insulin-dependent diabetes mellitus (NIDDM)) whose hyperglycaemia can no longer be controlled satisfactorily by diet, weight reduction and exercise. Repaglinide is also indicated in combination with metformin in type 2 diabetes patients who are not satisfactorily controlled on metformin alone. Treatment should be initiated as an adjunct to diet and exercise to lower the blood glucose in relation to meals.
- Product number
- EMEA/H/C/000187
- Authorisation holder
- Novo Nordisk A/S
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 4
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Diabetes Mellitus, Type 2
European medicines record
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- repaglinide
- Type
- Synthetic organic
- Drug name stem
- -glinide
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Mechanism
- Sulfonylurea receptor 1, Kir6.2 blocker
- Action type
- Blocker
- Target
- Sulfonylurea receptor 1, Kir6.2
- Protein identifier
- Q09428
- Mechanism
- Sulfonylurea receptor 1, Kir6.2 blocker
- Action type
- Blocker
- Target
- Sulfonylurea receptor 1, Kir6.2
- Protein identifier
- Q14654
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ATP-binding cassette, sub-family C (CFTR/MRP), member 8
- Gene symbol
- ABCC8
- Protein identifier
- Q09428
- Median affinity
- 6.97
- Affinity units
- pIC50
- Primary target
- Yes
Open Targets mechanisms
- Mechanism
- Sulfonylurea receptor 1, Kir6.2 blocker
- Action type
- Blocker
- Target
- Sulfonylurea receptor 1, Kir6.2
- Action type
- Blocker
- Gene symbol
- ABCC9|KCNJ11
- Protein identifier
- O60706|Q14654
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Blocker
- Gene symbol
- ABCC8|KCNJ11
- Protein identifier
- Q09428|Q14654
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Diabetes Mellitus
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000400
- Subject identifier
- D003920
- Condition
- Hypertension
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000537
- Subject identifier
- D006973
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Malaria
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001068
- Subject identifier
- D008288
- Condition
- Coronary Disease
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001645
- Subject identifier
- D003327
- Condition
- Atherosclerosis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003914
- Subject identifier
- D050197
- Condition
- Hypercholesterolemia
- Highest recorded phase
- 3
- Condition identifier
- HP:0003124
- Subject identifier
- D006937
- Condition
- Diabetes Mellitus, Type 2
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0005148
- Subject identifier
- D003924
- Condition
- Parkinson Disease
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0005180
- Subject identifier
- D010300
- Condition
- Prostatic Neoplasms, Castration-Resistant
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0008315
- Subject identifier
- D064129
- Condition
- Cystic Fibrosis
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0009061
- Subject identifier
- D003550
- Condition
- Anemia, Sickle Cell
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0011382
- Subject identifier
- D000755
- Condition
- Gastrointestinal Stromal Tumors
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0011719
- Subject identifier
- D046152
- Condition
- Mitochondrial Diseases
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0044970
- Subject identifier
- D028361
- Condition identifier
- EFO_0000400
- Condition identifier
- EFO_0009706
- Condition identifier
- EFO_0801077
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005015
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005148
- Condition identifier
- MONDO_0005148
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005180
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0006920
- Condition identifier
- MONDO_0008315
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0009061
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0011382
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0011719
- Highest recorded phase
- 1
- Event
- acute kidney injury
- Reports
- 141
- Reporting signal score
- 173.543
- Event
- agranulocytosis
- Reports
- 19
- Reporting signal score
- 18.7074
- Event
- anaemia haemolytic autoimmune
- Reports
- 9
- Reporting signal score
- 26.2838
- Event
- anuria
- Reports
- 15
- Reporting signal score
- 25.5934
- Event
- arthralgia
- Reports
- 2
- Reporting signal score
- 26.7502
- Event
- blood glucose increased
- Reports
- 34
- Reporting signal score
- 22.9759
- Event
- bradyphrenia
- Reports
- 20
- Reporting signal score
- 43.9638
- Event
- cardiac failure
- Reports
- 39
- Reporting signal score
- 35.4093
- Event
- cardio-respiratory arrest
- Reports
- 24
- Reporting signal score
- 47.8342
- Event
- cholestasis
- Reports
- 53
- Reporting signal score
- 99.6952
- Event
- confusional state
- Reports
- 78
- Reporting signal score
- 61.8267
- Event
- diabetes mellitus inadequate control
- Reports
- 34
- Reporting signal score
- 70.9808
- Event
- drug interaction
- Reports
- 75
- Reporting signal score
- 37.2945
- Event
- dysarthria
- Reports
- 36
- Reporting signal score
- 40.8638
- Event
- eosinophilia
- Reports
- 34
- Reporting signal score
- 54.7974
- Event
- erythromelalgia
- Reports
- 8
- Reporting signal score
- 33.9759
- Event
- fatigue
- Reports
- 8
- Reporting signal score
- 40.3164
- Event
- gamma-glutamyltransferase increased
- Reports
- 21
- Reporting signal score
- 18.4612
- Event
- glycosuria
- Reports
- 8
- Reporting signal score
- 21.7716
- Event
- haemoglobinuria
- Reports
- 8
- Reporting signal score
- 27.3264
- Event
- headache
- Reports
- 9
- Reporting signal score
- 28.5619
- Event
- hepatocellular injury
- Reports
- 34
- Reporting signal score
- 47.7059
- Event
- hyperglycaemia
- Reports
- 33
- Reporting signal score
- 39.1035
- Event
- hyperkalaemia
- Reports
- 52
- Reporting signal score
- 74.0841
- Event
- hyperthermia
- Reports
- 16
- Reporting signal score
- 26.4401
And 28 more, listed on the interactive page.
- NCT00000620
- NCT00118950
- NCT00118963
- NCT00336310
- NCT00399711
- NCT00491725
- NCT00568074
- NCT00568984
- NCT00799448
- NCT00819741
- NCT01022762
- NCT01465152
- NCT01489644
- NCT01490658
- NCT01562561
- NCT01605773
- NCT01698931
- NCT01709305
- NCT01720290
- NCT01720303
- NCT01780051
- NCT01919489
- NCT02040246
- NCT02694263
- NCT03359837
And 11 more, listed on the interactive page.
- Dose
- 0.5 mg to 4 mg
- Route
- Oral
- How often
- Before each meal
- Reduce dose if hypoglycemia occurs
- Skip dose if meal is skipped
- Take within 30 minutes before meals
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 2
- Polar surface area
- 78.87
- Calculated partition coefficient (ALogP)
- 5.22
- Calculated partition coefficient (XLogP)
- 5.2
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 10
- Heavy atoms
- 33
- Molecular formula
- C27H36N2O4
- Monoisotopic mass
- 452.26750763
- Natural product
- Yes
- 33342-248
- 33342-249
- 33342-250
- 57237-157
- 57237-158
- 57237-159
- 60687-560
- 62135-946
- 62135-947
- 62135-948
- 65862-670
- 65862-671
- 65862-672
- 72603-810
- 72603-811
- 72603-812
- 63629-4866
- 71335-2554
- 71335-2598
- 72162-2558
- Recorded assays
- 1,943
- Active assays
- 53
- Confirmatory
- Other
- Screening
- Summary
- Hypoglycemic Agents
These details could not be displayed.
Related records
Trials (70)
- A Clinical Drug-Drug Interaction (DDI) Study With Omaveloxolone
- A Double-Blind, Randomized, Parallel, Comparative Study to Evaluate the Efficacy and Safety of an Antidiabetic Agent Repaglinide for the Treatment of Type 2 Diabetes Mellitus Patients
- A Drug Drug Interaction Study to Evaluate the Effect of VCT220 on the Pharmacokinetics of Repaglinide, Rosuvastatin, and Digoxin in Healthy, Overweight, and Obese Subjects
- A Drug Interaction Study of LY3871801 in Healthy Participants
- A Drug-Drug Interaction (DDI) Study of HDM1002 With Repaglinide, Atorvastatin, Digoxin and Rosuvastatin in Healthy Subjects and Overweight Subjects.
- A Drug-Drug Interaction Study Evaluating the Perpetrator Potential of DC-806 on Cocktails of CYP450 Enzyme and Transporter Substrates in Healthy Participants
- A Drug-drug Interaction Study Evaluating the Perpetrator Potential of LY4100511 (DC-853) on Midazolam, Repaglinide, Digoxin, Rosuvastatin in Healthy Participants
- A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib
- A Drug-Drug Interaction Study to Evaluate the Effect of Ripretinib on the Pharmacokinetics of a CYP2C8 Probe Substrate in Patients with Advanced GIST
- A Drug-drug Interaction Study to Evaluate the Effects of Pelabresib on the Pharmacokinetics of Repaglinide, Midazolam, and Combined Oral Contraceptive in Patients With Advanced Malignancies
- A Pharmacokinetic Interaction Study Between Apatinib Mesylate and Repaglinide or Bupropion in Advanced Solid Tumor Subjects
- A Pharmacokinetic Study to Compare Co-administration of Repaglinide and Metformin HCl to Administration of Combination Preparation of Those Two Components
- A Pharmacokinetic Study to Evaluate the Drug Interaction Between SHR0302 and CYP Substrates in Healthy Volunteers
- A Study in Healthy Men and Women to Test Whether BI 1569912 Influences the Amount of Repaglinide, Midazolam and Bupropion in the Blood
- A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body
- A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants
- A Study of Imlunestrant (LY3484356) in Female Healthy Participants
- A Study of Neladalkib (NVL-655) in Patients With Advanced NSCLC and Other Solid Tumors Harboring ALK Rearrangement or Activating ALK Mutation (ALKOVE-1)
- A Study of the Effects of Pirtobrutinib (LOXO-305) on Repaglinide (CYP2C8 Substrate) in Healthy Participants
- A Study of the Interaction of Other Drugs With TAK-279 in Healthy Adults
Approved for (2)
In development for (12)
- Atherosclerosis Phase 3
- Coronary artery disorder Phase 3
- Cystic fibrosis Phase 3
- Gastrointestinal stromal tumor Phase 1
- Hypertensive disorder Phase 3
- Malaria Phase 1
- Mitochondrial disease Phase 1
- Neoplasm Phase 1
- Parkinson disease Phase 1
- Prostate cancer Phase 1
- Rheumatoid arthritis Phase 1
- Sickle cell disease Phase 1