Pregabalin

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

2004

www.ebi.ac.uk

First approval year: 2004
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Pregabalin
www.ebi.ac.uk

Molecular weight: 159.23
www.ebi.ac.uk

Structure (SMILES): CC(C)C[C@H](CN)CC(=O)O
www.ebi.ac.uk

alzain
Alzain
axalid
Axalid
bonqat
Bonqat
lecaent
Lecaent
lyrica
Lyrica
lyrica cr
Lyrica cr
pregabalin
Pregabalin
pregabalin accord
Pregabalin accord
pregabalin mylan
Pregabalin mylan
pregabalin mylan pharma
Pregabalin mylan pharma
pregabalin pfizer
Pregabalin pfizer
pregabalin sandoz
Pregabalin sandoz
pregabalin sandoz gmbh

And 7 more, listed on the interactive page.

150mg oral pregabalin capsule
300 mg pregabalin immediate release
75mg Pregabalin
ci 1008
CI-1008
lyrica
Lyrica
Lyrica (low dose)
Lyrica (pregabalin)
Lyrica 150Mg Capsule
Lyrica 300 mg
Lyrica CR (Pregabalin)
Lyrica®
Lyrica® (Pregabalin)
nsc 759256
NSC-759256
oral pregabalin
oral pregabalin 150 mg
pd 144723
PD-144723
pregabalin
Pregabalin
pregabalin (lyrica)
pregabalin (Lyrica)
pregabalin (LYRICA)

And 76 more, listed on the interactive page.

CAS registry numbers

148553-50-8

ChEMBL ID: CHEMBL1059
www.ebi.ac.uk

InChIKey: AYXYPKUFHZROOJ-ZETCQYMHSA-N
www.ebi.ac.uk

RxNorm IDs (RxCUI)

187832

FDA ingredient codes (UNII)

55JG375S6M

N02BF02
N03AX16

Sources for recorded values

www.ebi.ac.uk

5486971
25271887

Applicant: UPJOHN
Approval date: 30 Dec 2004
Application number: NDA021446

Status: Authorised
Status date: 5 Jul 2004
Authorisation date: 5 Jul 2004
Approved indications: Neuropathic pain Lyrica is indicated for the treatment of peripheral and central neuropathic pain in adults. Epilepsy Lyrica is indicated as adjunctive therapy in adults with partial seizures with or without secondary generalisation. Generalised anxiety disorder Lyrica is indicated for the treatment of generalised anxiety disorder (GAD) in adults.
Product number: EMEA/H/C/000546
Authorisation holder: Upjohn EESV
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

Anxiety Disorders
Epilepsy
Neuralgia

European medicines record

www.ema.europa.eu

Patents: 6
Designations: 0
Earliest recorded loss of exclusivity: 2 May 2027
First in class: No
Fast track: No
Breakthrough designation: No
Orphan designation: No
Priority review: No
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only

Pharmacology name: pregabalin
Type: Synthetic organic
Drug name stem: -gab-
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral

Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
O00305
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
O00555
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
O43497
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
O60359
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
O60840
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
O95180
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
P54284
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
P54289
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
P62955
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q00975
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q01668
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q02641
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q06432
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q08289
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q13698
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q13936
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q15878
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q7Z3S7
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q8IZS8
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q8WXS5
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q9BXT2
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q9NY47
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q9P0X4
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q9UBN1
Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel
Protein identifier
Q9UF02

And 1 more, listed on the interactive page.

Open Targets mechanisms

Mechanism
Voltage-gated calcium channel modulator
Action type
MODULATOR
Target
Voltage-gated calcium channel

Action type
MODULATOR
Gene symbol
CACNA2D1
Protein identifier
P54289
Organism
Homo sapiens
Target development level
Clinical
Action type
MODULATOR
Gene symbol
CACNA2D2
Protein identifier
Q9NY47
Organism
Homo sapiens
Target development level
Clinical

Condition
Pancreatitis, Chronic
Highest recorded phase
2
Condition identifier
EFO:0000342
Subject identifier
D050500
Condition
Diabetes Mellitus
Highest recorded phase
2
Condition identifier
EFO:0000400
Subject identifier
D003920
Condition
Epilepsy
Highest recorded phase
4
Condition identifier
EFO:0000474
Subject identifier
D004827
Condition
Irritable Bowel Syndrome
Highest recorded phase
2
Condition identifier
EFO:0000555
Subject identifier
D043183
Condition
Carcinoma, Squamous Cell
Highest recorded phase
1
Condition identifier
EFO:0000707
Subject identifier
D002294
Condition
Pregnancy
Highest recorded phase
1
Condition identifier
EFO:0002950
Subject identifier
D011247
Condition
Peripheral Nervous System Diseases
Highest recorded phase
3
Condition identifier
EFO:0003100
Subject identifier
D010523
Condition
Essential Tremor
Highest recorded phase
0.5
Condition identifier
EFO:0003108
Subject identifier
D020329
Condition
Tobacco Use Disorder
Highest recorded phase
0.5
Condition identifier
EFO:0003768
Subject identifier
D014029
Condition
Prostatitis
Highest recorded phase
3
Condition identifier
EFO:0003830
Subject identifier
D011472
Condition
Pain
Highest recorded phase
3
Condition identifier
EFO:0003843
Subject identifier
D010146
Condition
Fractures, Bone
Highest recorded phase
3
Condition identifier
EFO:0003931
Subject identifier
D050723
Condition
Peripheral Nervous System Diseases
Highest recorded phase
3
Condition identifier
EFO:0004149
Subject identifier
D010523
Condition
Neurotic Disorders
Highest recorded phase
3
Condition identifier
EFO:0004257
Subject identifier
D009497
Condition
Epilepsies, Partial
Highest recorded phase
3
Condition identifier
EFO:0004263
Subject identifier
D004828
Condition
Restless Legs Syndrome
Highest recorded phase
3
Condition identifier
EFO:0004270
Subject identifier
D012148
Condition
Sleep Initiation and Maintenance Disorders
Highest recorded phase
3
Condition identifier
EFO:0004698
Subject identifier
D007319
Condition
Anxiety
Highest recorded phase
3
Condition identifier
EFO:0005230
Subject identifier
D001007
Condition
Opioid-Related Disorders
Highest recorded phase
3
Condition identifier
EFO:0005611
Subject identifier
D009293
Condition
Fibromyalgia
Highest recorded phase
4
Condition identifier
EFO:0005687
Subject identifier
D005356
Condition
Neuralgia
Highest recorded phase
4
Condition identifier
EFO:0005762
Subject identifier
D009437
Condition
Herpes Zoster
Highest recorded phase
3
Condition identifier
EFO:0006510
Subject identifier
D006562
Condition
Anxiety Disorders
Highest recorded phase
4
Condition identifier
EFO:0006788
Subject identifier
D001008
Condition
Marijuana Abuse
Highest recorded phase
0.5
Condition identifier
EFO:0007191
Subject identifier
D002189
Condition
Epilepsy, Tonic-Clonic
Highest recorded phase
3
Condition identifier
EFO:0007262
Subject identifier
D004830

And 33 more, listed on the interactive page.

Condition identifier
EFO_0000182
Condition identifier
EFO_0000341
Condition identifier
EFO_0000342
Condition identifier
EFO_0000474
Condition identifier
EFO_0000555
Highest recorded phase
2
Condition identifier
EFO_0000707
Condition identifier
EFO_0002950
Highest recorded phase
1
Condition identifier
EFO_0003100
Highest recorded phase
2
Condition identifier
EFO_0003108
Condition identifier
EFO_0003768
Condition identifier
EFO_0003830
Highest recorded phase
3
Condition identifier
EFO_0003881
Highest recorded phase
3
Condition identifier
EFO_0003931
Highest recorded phase
3
Condition identifier
EFO_0004149
Highest recorded phase
3
Condition identifier
EFO_0004257
Highest recorded phase
3
Condition identifier
EFO_0004263
Highest recorded phase
3
Condition identifier
EFO_0004270
Highest recorded phase
3
Condition identifier
EFO_0004318
Highest recorded phase
1
Condition identifier
EFO_0004698
Highest recorded phase
3
Condition identifier
EFO_0005611
Highest recorded phase
3
Condition identifier
EFO_0005687
Condition identifier
EFO_0005762
Condition identifier
EFO_0005762
Highest recorded phase
4
Condition identifier
EFO_0006510
Highest recorded phase
3
Condition identifier
EFO_0006788

And 85 more, listed on the interactive page.

Event
coma
Reports
821
Reporting signal score
708.26
Event
confusional state
Reports
2,726
Reporting signal score
1,754.86
Event
dizziness
Reports
4,445
Reporting signal score
1,311.3
Event
drug abuse
Reports
2,172
Reporting signal score
2,470.66
Event
drug dependence
Reports
970
Reporting signal score
1,067.96
Event
drug hypersensitivity
Reports
7,198
Reporting signal score
7,092.31
Event
fall
Reports
2,230
Reporting signal score
728.844
Event
feeling abnormal
Reports
2,513
Reporting signal score
1,664.89
Event
fibromyalgia
Reports
454
Reporting signal score
622.35
Event
gait disturbance
Reports
1,384
Reporting signal score
765.181
Event
insomnia
Reports
2,401
Reporting signal score
1,016.64
Event
memory impairment
Reports
1,004
Reporting signal score
703.111
Event
myoclonus
Reports
857
Reporting signal score
1,283.28
Event
pain
Reports
5,616
Reporting signal score
2,682.03
Event
pain in extremity
Reports
1,822
Reporting signal score
635.639
Event
somnolence
Reports
4,637
Reporting signal score
4,749.1
Event
therapeutic product effect incomplete
Reports
698
Reporting signal score
662.691
Event
vision blurred
Reports
1,234
Reporting signal score
802.377
Event
weight increased
Reports
2,719
Reporting signal score
1,824.67
Event
withdrawal syndrome
Reports
1,691
Reporting signal score
2,778.35

NCT00141219
clinicaltrials.gov
NCT00141401
clinicaltrials.gov
NCT00143156
clinicaltrials.gov
NCT00150423
clinicaltrials.gov
NCT00553280
clinicaltrials.gov
NCT00553475
clinicaltrials.gov
NCT00643760
clinicaltrials.gov
NCT00785577
clinicaltrials.gov
NCT00837941
clinicaltrials.gov
NCT00870454
clinicaltrials.gov
NCT01057693
clinicaltrials.gov
NCT01089556
clinicaltrials.gov
NCT01332149
clinicaltrials.gov
NCT01455415
clinicaltrials.gov
NCT01474772
clinicaltrials.gov
NCT01496365
clinicaltrials.gov
NCT01863810
clinicaltrials.gov
NCT01928381
clinicaltrials.gov
NCT02215252
clinicaltrials.gov
NCT02372578
clinicaltrials.gov
NCT05660538
clinicaltrials.gov
NCT00150436
clinicaltrials.gov
NCT00292188
clinicaltrials.gov
NCT00407745
clinicaltrials.gov
NCT00631943
clinicaltrials.gov

And 164 more, listed on the interactive page.

Dose: 150 mg/day
Route: Oral
How often: Twice daily or three times daily

Hydrogen bond acceptors: 2
Hydrogen bond donors: 2
Polar surface area: 63.32
Calculated partition coefficient (ALogP): 1.08
Calculated partition coefficient (XLogP): -0.9
Prodrug: No
Chirality: Single enantiomer
Inorganic: No
Rule-of-five violations: 0
Rotatable bonds: 5
Heavy atoms: 11
Molecular formula: C8H17NO2
Monoisotopic mass: 159.125928785
Natural product: Yes

0071-1018
0904-6991
0904-6992
0904-7000
0904-7001
0904-7002
0904-7003
0904-7004
0904-7005
13668-358
13668-359
13668-360
13668-361
13668-362
13668-363
13668-364
13668-365
14445-123
14445-124
14445-125
14445-126
14445-127
14445-128
14445-173
14445-174

And 514 more, listed on the interactive page.

Recorded assays: 576
Active assays: 21

Active assay types

Confirmatory

Analgesics
id.nlm.nih.gov
Anticonvulsants
id.nlm.nih.gov
Calcium Channel Blockers
id.nlm.nih.gov
Anti-Anxiety Agents
id.nlm.nih.gov

Oral bioavailability

Median: 85.5
Mean: 85.5
Minimum: 83
Maximum: 88
Unit: %
Assays: 2
Standard deviation: 3.53553
Summary method: median
Censored results excluded: 0
Other units excluded: 0
Unknown units excluded: 0

Measurement types

Related records

Trials (553)

'Fix the Dysfunction' Concept for Mechanism-based Pharmacological Treatment of Neuropathic Pain by Drug
[S,S]-Reboxetine Add-On Trial
12-Week Efficacy And Safety Of Pregabalin In Treating Restless Legs Syndrome (RLS) Subjects
600 mg Amoxicillin/42.9 mg Clavulanate Postassium /5 mL Suspension Under Fasting Conditions
A 12-Month Study To Evaluate The Safety And Tolerability Of Pregabalin As Add-On Therapy In Pediatric Subjects 1 Month To 16 Years Of Age With Partial Onset Seizures And Pediatric And Adult Subjects 5 To 65 Years Of Age With Primary Generalized Tonic-Clonic Seizures
A 13-Week, Randomized, Double-Blind, Multicenter, Placebo-Controlled Study Of Pregabalin For Postherpetic Neuralgia
A 17-Week Trial To Assess Pregabalin For The Treatment Of Nerve Pain Due To Spinal Cord Injury
A 2-part Study to Assess Local Tolerability, Safety and Pharmacokinetics of Ceftaroline in Healthy Subjects
A 2-part Trial to Learn More About How BAY1817080 Works, How Safe it is, and What the Right Dose is for Participants With Diabetic Neuropathic Pain
A 2x2 Factorial, Randomized, Open-label Trial to Evaluate Neuromodulators and Cough Control Therapy in Patients With Refractory or Unexplained Chronic Cough
A Clinical Trial to Compare The Pharmacokinetics of A Pregabalin GLARS Tablet 150mg With Immediate Release Formulation and to Assess The Effect of High Fat Diet in Healthy Male Subjects
A Clinical Trial to Compare The Pharmacokinetics of A Pregabalin GLARS-NF1 Tablet 150mg With Immediate Release Formulation and to Assess The Effect of High Fat Diet in Healthy Male Subjects
A Clinical Trial To Evaluate PF-05089771 On Its Own And As An Add-On Therapy To Pregabalin (Lyrica) For The Treatment Of Pain Due To Diabetic Peripheral Neuropathy (DPN)
A Clinical Trial to Evaluate the Efficacy and Safety of HL-1186 Tablet in the Treatment of Postherpetic Neuralgia
A Comparison of Pregabalin (Lyrica®) to Placebo in Pain Relief After Photorefractive Keratectomy (PRK) Surgery
A Controlled Pregabalin Trial In Fibromyalgia
A Long-Term Study To Evaluate Safety And Efficacy Of Pregabalin For Pain Associated With Diabetic Peripheral Neuropathy
A Long-Term Study To Evaluate Safety And Efficacy Of Pregabalin For Postherpetic Neuralgia
A Long-Term Study To Evaluate Safety And Efficacy Of Pregabalin In Patients With Fibromyalgia
A Methodology Study Of Brain Imaging Of Pain-Killers In Post-Traumatic Neuropathic Pain Patients

Approved for (7)

Anxiety disorder
Epilepsy
Fibromyalgia
Generalized anxiety disorder
Neuralgia
Spinal cord injury
Visual epilepsy

In development for (38)

Alcohol dependence Phase 2
Anxiety Phase 3
Bone fracture Phase 3
Breast cancer Phase 3
Burning mouth syndrome Phase 3
Cannabis dependence Early phase 1
Chronic pancreatitis Phase 2
Complex partial epilepsy Phase 3
Complex regional pain syndrome Phase 2
Dementia Phase 3
Depressive disorder Phase 3
Diabetes mellitus Phase 2
Diabetic neuropathy Phase 3
Dry eye syndrome Phase 2
Epilepsy with generalized tonic-clonic seizures Phase 3
Essential tremor Early phase 1
Focal epilepsy Phase 3
Herpes zoster Phase 3
Insomnia Phase 3
Intervertebral disk degenerative disorder Phase 3

Targets (26)

CACNA1A Voltage-gated calcium channel modulator
CACNA1B Voltage-gated calcium channel modulator
CACNA1C Voltage-gated calcium channel modulator
CACNA1D Voltage-gated calcium channel modulator
CACNA1E Voltage-gated calcium channel modulator
CACNA1F Voltage-gated calcium channel modulator
CACNA1G Voltage-gated calcium channel modulator
CACNA1H Voltage-gated calcium channel modulator
CACNA1I Voltage-gated calcium channel modulator
CACNA1S Voltage-gated calcium channel modulator
CACNA2D1 Voltage-gated calcium channel modulator
CACNA2D2 Voltage-gated calcium channel modulator
CACNA2D3 Voltage-gated calcium channel modulator
CACNA2D4 Voltage-gated calcium channel modulator
CACNB1 Voltage-gated calcium channel modulator
CACNB2 Voltage-gated calcium channel modulator
CACNB3 Voltage-gated calcium channel modulator
CACNB4 Voltage-gated calcium channel modulator
CACNG1 Voltage-gated calcium channel modulator
CACNG2 Voltage-gated calcium channel modulator

Pregabalin

Development status

Names and chemistry

Brand names (32)

Other names (101)

Identifiers

ATC classification codes (2)

PubChem compound IDs (2)

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (26)

Open Targets mechanisms

DrugCentral mechanisms (2)

Investigated indications (58)

Open Targets indications (110)

Reported adverse events (20)

Trial references (189)

Dosing

Chemical properties

National Drug Codes

Evidence counts

Active assay types

Pharmacologic actions

Biological measurements

Observed measurements

Oral bioavailability

Measurement types

Related records

Trials (553)

Approved for (7)

In development for (38)

Other linked conditions (5)

Targets (26)