> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/repaglinide-079ab94a-0782-4b94-b6e7-73df134ff710
> Record changed: 2026-10-13

# Repaglinide

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

First approval year

1997

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

## Development status

**First approval year**

1997

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**Drug name**

Repaglinide

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**Molecular weight**

452.6

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**Structure (SMILES)**

CCOc1cc(CC(=O)N\[C@@H\](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

### Brand names (16)

- 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

### Other names (65)

- (+)-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.

## Identifiers

**ATC classification codes**

- A10BX02

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**CAS registry numbers**

- 135062-02-1

**ChEMBL ID**

CHEMBL1272

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**InChIKey**

FAEKWTJYAYMJKF-QHCPKHFHSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1272)

**PubChem compound IDs**

- 65981

**RxNorm IDs (RxCUI)**

- 73044

**FDA ingredient codes (UNII)**

- 668Z8C33LU

## Regulatory information

### United States

**Applicant**

GEMINI LABS LLC

**Approval date**

22 Dec 1997

**Application number**

NDA020741

### European Union

**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

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/novonorm)

### Other regulatory facts

**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

### Drug classification

**Pharmacology name**

repaglinide

**Type**

Synthetic organic

**Drug name stem**

\-glinide

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (3)

- **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

### DrugCentral mechanisms (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

### Investigated indications (15)

- **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

### Open Targets indications (12)

- **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

### Reported adverse events (53)

- **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.

### Trial references (36)

- NCT00000620  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000620)
- NCT00118950  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00118950)
- NCT00118963  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00118963)
- NCT00336310  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00336310)
- NCT00399711  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00399711)
- NCT00491725  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00491725)
- NCT00568074  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00568074)
- NCT00568984  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00568984)
- NCT00799448  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00799448)
- NCT00819741  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00819741)
- NCT01022762  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01022762)
- NCT01465152  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01465152)
- NCT01489644  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01489644)
- NCT01490658  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01490658)
- NCT01562561  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01562561)
- NCT01605773  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01605773)
- NCT01698931  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01698931)
- NCT01709305  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01709305)
- NCT01720290  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01720290)
- NCT01720303  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01720303)
- NCT01780051  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01780051)
- NCT01919489  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01919489)
- NCT02040246  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02040246)
- NCT02694263  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02694263)
- NCT03359837  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03359837)

And 11 more, listed on the interactive page.

## Dosing

**Dose**

0.5 mg to 4 mg

**Route**

Oral

**How often**

Before each meal

### Conditions of use (3)

- Reduce dose if hypoglycemia occurs
- Skip dose if meal is skipped
- Take within 30 minutes before meals

## Chemical properties

**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

## National Drug Codes

- 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

## Evidence counts

**Recorded assays**

1,943

**Active assays**

53

### Active assay types (4)

- Confirmatory
- Other
- Screening
- Summary

## Pharmacologic actions

- Hypoglycemic Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D007004.html)

## Biological measurements

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)](https://trialight.com/data/trial/a-study-of-neladalkib-nvl-655-in-patients-with-advanced-56190eab-981f-4038-b03b-4ccae9704b2a.md)
- 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)

- [Diabetes mellitus](https://trialight.com/data/condition/diabetes-mellitus-1a0391a8-9f84-5600-a2bf-ec97c2229de4.md)
- [Type 2 diabetes mellitus](https://trialight.com/data/condition/type-2-diabetes-mellitus-98e14a90-bb06-5174-90c7-901a0a259fb9.md)

### In development for (12)

- [Atherosclerosis](https://trialight.com/data/condition/atherosclerosis-5dab64e9-1fd4-5dd2-90c2-ce84935652d1.md) Phase 3
- [Coronary artery disorder](https://trialight.com/data/condition/coronary-artery-disorder-6f736849-d477-587a-b3fa-b0621d573407.md) Phase 3
- [Cystic fibrosis](https://trialight.com/data/condition/cystic-fibrosis-6f9870eb-6ebc-5bec-a50b-34b0b323a7c3.md) Phase 3
- [Gastrointestinal stromal tumor](https://trialight.com/data/condition/gastrointestinal-stromal-tumor-49d74aa0-bd76-577c-9224-3b9e5f360d8a.md) Phase 1
- [Hypertensive disorder](https://trialight.com/data/condition/hypertensive-disorder-6d786557-b9e8-5afc-80f3-89a1995f9da5.md) Phase 3
- [Malaria](https://trialight.com/data/condition/malaria-54828cac-9b96-5833-93e2-e012d4505853.md) Phase 1
- Mitochondrial disease Phase 1
- Neoplasm Phase 1
- [Parkinson disease](https://trialight.com/data/condition/parkinson-disease-a117728d-ad75-551b-9b20-fffa9a2305ac.md) Phase 1
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 1
- [Rheumatoid arthritis](https://trialight.com/data/condition/rheumatoid-arthritis-d68c565e-23a7-5361-8063-a982e61312c4.md) Phase 1
- Sickle cell disease Phase 1

### Targets (2)

- [ABCC8](https://trialight.com/data/target/abcc8-d5b12ce5-01cf-50d6-9a80-43fb995d8808.md) Sulfonylurea receptor 1, Kir6.2 blocker
- [KCNJ11](https://trialight.com/data/target/kcnj11-0c4c8434-214d-5b32-815c-56501b745a8a.md) Sulfonylurea receptor 1, Kir6.2 blocker

---

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