Pregabalin

Summary

Pregabalin (CHEMBL1059) is an approved small-molecule anticonvulsant (ATC N02BF02); indicated across 57 conditions including fibromyalgia and visual epilepsy.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02BF02
• Indications: 57 conditions
• Clinical trials: 451
• Chemistry: 159.23 Da · C8H17NO2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1059
Name	Pregabalin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5486971
ChEBI	CHEBI:64356
ATC	N02BF02
Molecular formula	C8H17NO2
Molecular weight	159.23
InChIKey	AYXYPKUFHZROOJ-ZETCQYMHSA-N

SMILES: CC(C)C[C@@H](CC(=O)O)CN

IUPAC name: (3S)-3-(aminomethyl)-5-methylhexanoic acid

ChEBI definition: A γ-amino acid that is γ-aminobutyric acid (GABA) carrying an isobutyl substitutent at the β-position (the S-enantiomer). Binds with high affinity to the α2-δ site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.

Pharmacological roles (ChEBI): anticonvulsant, calcium channel blocker.

Also known as: Alzain, Axalid, Bonqat, CI-1008, Lecaent, Lyrica, Lyrica cr, NSC-759256, PD-144723, Pregabalin, Pregabalin accord, Pregabalin mylan

Patent coverage: 6,972 distinct patent families (26,074 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Voltage-dependent calcium channel subunit alpha-2/delta-1, Progesterone receptor, Alpha-1A adrenergic receptor, Voltage-dependent calcium channel subunit alpha-2/delta-2.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CACNA2D1	7.72	Ki	19	nM	CHEMBL_ACT_22812944
CACNA2D1	7.72	Ki	19	nM	CHEMBL_ACT_23226778
CACNA2D2	7	Ki	99	nM	CHEMBL_ACT_22812955
ADRA1A	5.43	AC50	3672	nM	CHEMBL_ACT_25138238

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

57 indications (9 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
fibromyalgia	4	MONDO:0005546	EFO:0005687
visual epilepsy	4	MONDO:0001386	HP:0001250
epilepsy	4	MONDO:0005027	EFO:0000474
neuralgia	4	MONDO:0021667	EFO:0005762
generalized anxiety disorder	4	MONDO:0001942	EFO:1001892
spinal cord injury	4	MONDO:0043797	EFO:1001919
anxiety disorder	4	MONDO:0005618	EFO:0006788
peripheral nervous system disorder	3	MONDO:0003620	EFO:0004149
focal epilepsy	3	MONDO:0005384	EFO:0004263
restless legs syndrome	3	MONDO:0005391	EFO:0004270
anxiety	3	MONDO:0011918	EFO:0005230
bone fracture	3	MONDO:0005315	EFO:0003931
complex partial epilepsy	3	MONDO:0006710	EFO:1000877
diabetic neuropathy	3	MONDO:0006626	EFO:1000783
neurotic disorder	3	MONDO:0005379	EFO:0004257
dementia	3	MONDO:0001627	HP:0000726
peripheral neuropathy	3	MONDO:0005244	EFO:0003100
mononeuropathy	3	MONDO:0001397	EFO:0009558
insomnia	3	MONDO:0013600	EFO:0004698
opiate dependence	3	MONDO:0005530	EFO:0005611
epilepsy with generalized tonic-clonic seizures	3	MONDO:0005754	HP:0002069
intervertebral disk degenerative disorder	3	MONDO:0011385	HP:0008419
radiculopathy	3	MONDO:0002959	MONDO:0002959
breast neoplasm	3	MONDO:0021100	MONDO:0007254
prostatitis	3	MONDO:0005280	EFO:0003830
herpes zoster	3	MONDO:0005609	EFO:0006510
depressive disorder	3	MONDO:0002050	MONDO:0002050
osteoarthritis	3	MONDO:0005178	MONDO:0005178
migraine disorder	3	MONDO:0005277	MONDO:0005277
burning mouth syndrome	3	MONDO:0006687	EFO:1000850
irritable bowel syndrome	2	MONDO:0005052	EFO:0000555
chronic pancreatitis	2	MONDO:0005003	EFO:0000342
dry eye syndrome	2	MONDO:0006733	EFO:1000906
overactive bladder	2	MONDO:0006624	EFO:1000781
diabetes mellitus	2	MONDO:0005015	EFO:0000400
complex regional pain syndrome	2	MONDO:0019369	EFO:1001998
alcohol abuse	2	MONDO:0002046	MONDO:0007079
squamous cell carcinoma	1	MONDO:0005096	EFO:0000707
oropharynx cancer	1	MONDO:0004608	EFO:1001931
refractive error	1	MONDO:0004892	MONDO:0004892
nicotine dependence	0	MONDO:0008575	EFO:0003768
cannabis dependence	0	MONDO:0005689	EFO:0007191
essential tremor	0	MONDO:0003233	EFO:0003108

14 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 451.

Phase distribution

Phase	Trials
PHASE4	124
PHASE3	117
Not specified	90
PHASE2	64
PHASE1	29
PHASE2/PHASE3	12
EARLY_PHASE1	9
PHASE1/PHASE2	6

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05488847	PHASE4	ACTIVE_NOT_RECRUITING	Opioid-Free Pain Protocol After Shoulder Arthroplasty
NCT05640453	PHASE4	RECRUITING	Pregabalin Versus Dexmedetomidine for Delirium Treatment After Coronary Artery Bypass Grafting
NCT05804591	PHASE4	RECRUITING	Pregabalin in the Obese Patients Undergoing Laparoscopic Sleeve Gastrectomy (LSG).
NCT06367998	PHASE4	NOT_YET_RECRUITING	Effect of Pregabalin on Shoulder Pain in Patients With Central Sensitization After Arthroscopic Rotator Cuff Repair
NCT06790537	PHASE4	RECRUITING	Efficacy of Pregabalin for Diabetic Pruritus - A Randomized Controlled Study.
NCT07288528	PHASE4	NOT_YET_RECRUITING	A 2x2 Factorial, Randomized, Open-label Trial to Evaluate Neuromodulators and Cough Control Therapy in Patients With Refractory or Unexplained Chronic Cough
NCT07451431	PHASE4	RECRUITING	Efficacy and Safety of Mirogabalin in Diabetic Peripheral Neuropathic Pain
NCT07567924	PHASE4	ACTIVE_NOT_RECRUITING	Comparison Between Pregabalin and Acetaminophen for the Treatment of Post-Mastectomy Pain Syndrome
NCT00141427	PHASE4	COMPLETED	Pregabalin In Partial Seizures: An Open-Label, International, Multicenter Add-On Therapy Trial.
NCT00156078	PHASE4	COMPLETED	A Study To Evaluate Pregabalin In Patients With Painful Diabetic Peripheral Neuropathy (DPN)
NCT00159666	PHASE4	COMPLETED	Study of Pregabalin Therapy for Pain Relief in Subjects With Post-Herpetic Neuralgia
NCT00159679	PHASE4	COMPLETED	Pregabalin in the Treatment of Pain Due to Diabetic Peripheral Neuropathy
NCT00159731	PHASE4	COMPLETED	Safety of Pregabalin in the Treatment of Pain Due to Diabetic Peripheral Neuropathy
NCT00235261	PHASE4	COMPLETED	Effect of Paracetamol, Pregabalin and Dexamethasone on Pain and Opioid Requirements in Patients After Hip Operations
NCT00288639	PHASE4	COMPLETED	Lyrica (Pregabalin) Administered as an Add-on Therapy for Partial Seizures (LEADER).
NCT00292188	PHASE4	COMPLETED	P4 (Pregabalin for Peripheral Posttraumatic Pain)
NCT00310583	PHASE4	UNKNOWN	Effects of Pregabalin on Mechanical Hyperalgesia
NCT00313820	PHASE4	COMPLETED	Efficacy Of Pregabalin In Subjects With Post-Stroke Central Neuropathic Pain
NCT00351611	PHASE4	COMPLETED	Vision Testing in Patients With Partial Seizures Receiving Either Lyrica or Placebo
NCT00353704	PHASE4	COMPLETED	Analgetic and Anxiolytic Effect of Preoperative Pregabalin
NCT00378547	PHASE4	TERMINATED	Effect of Paracetamol, Pregabalin and Dexamethasone on Pain and Opioid Requirements in Patients Having a Tonsillectomy
NCT00380874	PHASE4	TERMINATED	Prevention And Treatment Of Chemotherapy-Induced Peripheral Neuropathy In Subjects With Advanced Colorectal Cancer
NCT00381095	PHASE4	TERMINATED	A Study To Evaluate Pregabalin In The Treatment Of Moderate To Severe Chronic Bone Pain Related To Metastatic Cancer
NCT00385671	PHASE4	COMPLETED	An Open-Label Comparison of Duloxetine to Other Alternatives for the Management of Diabetic Peripheral Neuropathic Pain
NCT00403780	PHASE4	TERMINATED	Randomized Study of Pregabalin for Pain Reduction in Patients With Rest Pain and Lower Limb Ischemia
NCT00407511	PHASE4	COMPLETED	Pregabalin Treatment Of Peripheral Neuropathic Pain Associated With Diabetic Peripheral NeP (DPN), Postherpetic Neuralgia (PHN), HIV-related NeP (HIV), and Chemotherapy Induced NeP
NCT00407797	PHASE4	TERMINATED	Pregabalin In Partial Seizures (PREPS): An Open-Label, Multicenter Add On Therapy Trial
NCT00537940	PHASE4	COMPLETED	Comparative Study Of Pregabalin And Gabapentin As Adjunctive Therapy In Subjects With Partial Seizures
NCT00573261	PHASE4	COMPLETED	A Randomized Double-Blind Study Testing the Effects of Pregabalin on Diabetic Neuropathy
NCT00584246	PHASE4	WITHDRAWN	Pregabalin (Lyrica) for the Treatment of Restless Legs Syndrome
NCT00584376	PHASE4	COMPLETED	Pregabalin (Lyrica) for the Treatment of Essential Tremor
NCT00624780	PHASE4	COMPLETED	Safety and Efficacy Evaluation Of Pregabalin (Lyrica) With Patients With Generalized Anxiety Disorder
NCT00629681	PHASE4	COMPLETED	A Study of the Efficacy and Safety of Pregabalin for the Treatment of Diabetic Peripheral Neuropathy or Postherpetic Neuralgia
NCT00631696	PHASE4	COMPLETED	Evaluation Of Sperm Production With Healthy Male Volunteers Receiving Lyrica Or Placebo
NCT00638443	PHASE4	COMPLETED	Lumbar Stenosis Outcomes Research (LUSTOR)
NCT00663962	PHASE4	COMPLETED	Pregabalin and Post-thoracotomy Pain
NCT00706836	PHASE4	COMPLETED	PharmacofMRI of Anxiolytic Medications (Pregabalin)
NCT00762099	PHASE4	UNKNOWN	Perioperative Pregabalin Use, Rehabilitation, Pain Outcomes and Anxiety Following Hip Surgery
NCT00781131	PHASE4	COMPLETED	Trial of Pregabalin for Post-operative Pain in Women Undergoing Abdominal Hysterectomy
NCT00785382	PHASE4	COMPLETED	Pregabalin for Postoperative Pain in Women Undergoing Breast Cancer Surgery

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 6 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).