Active Ingredient History
Gabapentin enacarbil (Horizant in USA, Regnite in Japan), is a prodrug of gabapentin, an antiepileptic drug (AED). It was designed for increased oral bioavailability over gabapentin and to be transported through two high capacity transporters in the intestine, sodium-dependent multivitamin transporter (SMVT) and MCT1. It was shown that the prodrug is a substrate for both MCT1 and SMVT. The oral bioavailability of gabapentin following the administration of its prodrug was found to be 84.2% compared with 25.4% after a similar oral dose of gabapentin. Discovered and developed by XenoPort, gabapentin enacarbil was approved in the United States in 2011 for the treatment of moderate-to-severe primary restless legs syndrome (RLS) in adults and in June 2012 for the management of postherpetic neuralgia (PHN) in adults. Therapeutic effects of gabapentin enacarbil in RLS and PHN are attributable to gabapentin. The precise mechanism by which gabapentin is efficacious in RLS and PHN is unknown. In vitro studies have shown that gabapentin binds with high affinity to certain parts of voltage-activated calcium channels in the central nervous system. However, the relationship of this binding to the therapeutic effects of gabapentin enacarbil in RLS and PHN is unknown. The most common adverse reactions for adult patients with moderate-to-severe primary RLS and PHN receiving Horizant were somnolence/sedation, dizziness, headache, nausea and fatigue. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Abortion, Induced (Phase 2)
Abortion, Spontaneous (Phase 2)
Acinetobacter Infections (Phase 1/Phase 2)
Acute Pain (Phase 4)
Alcohol Drinking (Phase 3)
Alcohol-Induced Disorders (Phase 2)
Alcoholism (Phase 4)
Alcohol Withdrawal Delirium (Phase 4)
Alopecia (Early Phase 1)
Alzheimer Disease (Phase 4)
Amputation (Phase 4)
Analgesia (Phase 4)
Analgesics (Phase 4)
Analgesics, Opioid (Phase 4)
Anemia, Sickle Cell (Phase 2)
Anesthesia (Phase 4)
Anesthesia, General (Phase 3)
Anterior Cruciate Ligament Injuries (Phase 2/Phase 3)
Anxiety (Phase 4)
Anxiety Disorders (Phase 3)
Arthralgia (Phase 2/Phase 3)
Arthritis (Phase 4)
Arthroplasty (Phase 4)
Arthroplasty, Replacement, Knee (Phase 4)
Arthroscopy (Phase 4)
Asthma (Phase 4)
Autism Spectrum Disorder (Phase 4)
Back Pain (Phase 2)
Bipolar Disorder (Phase 2)
Blood Pressure (Phase 4)
Breast Neoplasms (Phase 3)
Cannabis (Phase 2)
Carcinoma, Squamous Cell (Phase 2)
Cardiopulmonary Bypass (Phase 4)
Carpal Tunnel Syndrome (Phase 4)
Cerebral Palsy (Phase 4)
Cesarean Section (Phase 4)
Chest Pain (Phase 4)
Cholecystectomy, Laparoscopic (Phase 4)
Cholecystolithiasis (Phase 4)
Cholestasis (Phase 3)
Chronic Pain (Phase 4)
Cigarette Smoking (Phase 2)
Cocaine-Related Disorders (Phase 2)
Cognition Disorders (Phase 2)
Colitis, Ulcerative (Phase 4)
Colonic Neoplasms (Phase 4)
Colorectal Surgery (Phase 3)
Complex Regional Pain Syndromes (Phase 4)
Conscious Sedation (Phase 4)
Constipation (Phase 4)
Crying (Phase 4)
Cystitis, Interstitial (Phase 4)
Dementia (Phase 3)
Depression (Phase 3)
Dermatology (Early Phase 1)
Dexmedetomidine (Phase 3)
Diabetes Mellitus (Phase 2)
Diabetes Mellitus, Type 2 (Phase 4)
Diabetic Foot (Phase 1/Phase 2)
Diabetic Neuropathies (Phase 4)
Diverticulitis, Colonic (Phase 4)
Drug Misuse (Phase 1)
Drug Resistant Epilepsy (Phase 4)
Drugs, Investigational (Phase 2)
Dyspepsia (Phase 3)
Epilepsies, Partial (Phase 4)
Epilepsy ()
Epilepsy, Complex Partial (Phase 4)
Epinephrine (Phase 4)
Essential Tremor (Phase 4)
Fabry Disease (Phase 2)
Facial Pain (Phase 4)
Fibromyalgia (Phase 3)
Fibrosis (Phase 3)
Fractures, Bone (Phase 4)
Gabapentin (Phase 4)
General Surgery (Phase 4)
Genital Diseases, Female (Phase 2/Phase 3)
Glioma (Phase 4)
Hand Injuries (Phase 4)
Head and Neck Neoplasms (Phase 4)
Healthy Volunteers (Phase 4)
Hernia (Phase 4)
Hernia, Inguinal (Phase 2/Phase 3)
Herpes Zoster (Phase 4)
HIV Infections (Phase 4)
Hospitalization (Phase 3)
Hot Flashes (Phase 4)
Hyperalgesia (Phase 4)
Hyperemesis Gravidarum (Phase 3)
Hypertension (Early Phase 1)
Hysterectomy (Phase 4)
Ileus (Phase 4)
Infant, Premature (Phase 1)
Infertility, Male (Phase 3)
Intervertebral Disc Displacement (Phase 2)
Intestinal Pseudo-Obstruction (Phase 4)
Intubation (Phase 2/Phase 3)
Irritable Bowel Syndrome (Phase 4)
Irritable Mood (Phase 2)
Ischemic Stroke (Phase 3)
Ketamine (Phase 3)
Kidney Diseases (Phase 4)
Kidney Failure, Chronic (Phase 4)
Laparoscopy (Phase 3)
Lichen Planus (Early Phase 1)
Lidocaine (Phase 3)
Liver Cirrhosis (Phase 3)
Liver Diseases (Phase 3)
Lung Diseases (Phase 3)
Lung Neoplasms (Phase 3)
Marijuana Abuse (Phase 2)
Meniscus (Early Phase 1)
Menopause (Phase 3)
Mental Health (Phase 1/Phase 2)
Migraine Disorders (Phase 2)
Mood Disorders (Phase 2)
Mucositis (Phase 3)
Multiple Sclerosis (Phase 2)
Muscle Weakness (Phase 2/Phase 3)
Musculoskeletal Diseases (Phase 4)
Myalgia (Phase 2/Phase 3)
Narcotics (Phase 4)
Nausea (Phase 4)
Neoplasms (Phase 3)
Nerve Degeneration (Phase 4)
Neuralgia (Phase 4)
Neuralgia, Postherpetic (Phase 4)
Nocturia (Phase 2/Phase 3)
Nystagmus, Pathologic (Phase 4)
Opioid-Related Disorders (Phase 4)
Oropharyngeal Neoplasms (Phase 3)
Orthopedics (Phase 4)
Osteoarthritis (Phase 4)
Osteoarthritis, Knee (Phase 4)
Oximetry (Phase 3)
Pain (Phase 4)
Pain Management (Phase 4)
Pain, Postoperative (Phase 4)
Paresthesia (Phase 4)
Pathologic Processes (Phase 3)
Pelvic Organ Prolapse (Phase 4)
Pelvic Pain (Phase 4)
Peripheral Nerve Injuries (Phase 4)
Peripheral Nervous System Diseases (Phase 4)
Pharmacokinetics (Phase 3)
Polyneuropathies (Phase 3)
Post-Dural Puncture Headache (Phase 4)
Postoperative Complications (Phase 3)
Postoperative Nausea and Vomiting (Phase 4)
Postpartum Period (Phase 4)
Prostatic Neoplasms (Phase 4)
Prostatitis (Phase 4)
Pruritus (Phase 4)
Pseudomonas Infections (Phase 1/Phase 2)
Psychophysiologic Disorders (Phase 3)
Psychotic Disorders (Phase 2)
Quality of Life (Phase 3)
Radiation Oncology (Phase 3)
Radiculopathy (Phase 4)
Rectal Neoplasms (Phase 4)
Respiratory Insufficiency (Phase 3)
Rib Fractures (Phase 4)
Rotator Cuff Injuries (Phase 4)
Schizophrenia (Phase 3)
Scoliosis (Phase 3)
Seizures (Phase 3)
Signs and Symptoms, Digestive (Phase 2)
Sleep (Phase 4)
Sleep Apnea, Obstructive (Phase 3)
Sleep Apnea Syndromes (Phase 3)
Sleep Disorders, Intrinsic (Phase 2)
Sphenopalatine Ganglion Block (Phase 4)
Spinal Cord Injuries (Phase 4)
Spinal Diseases (Phase 3)
Spinal Stenosis (Phase 4)
Squamous Cell Carcinoma of Head and Neck (Phase 3)
Staphylococcal Infections (Phase 1/Phase 2)
Subarachnoid Hemorrhage (Phase 4)
Substance Abuse, Oral (Phase 4)
Substance-Related Disorders (Phase 2/Phase 3)
Thoracic Injuries (Phase 3)
Thoracic Surgery (Phase 4)
Tinnitus (Phase 2/Phase 3)
Tobacco Use (Phase 2)
Tonsillectomy (Phase 4)
Tonsillitis (Phase 4)
Urethral Obstruction (Phase 4)
Urethral Stricture (Phase 4)
Urinary Bladder (Phase 2/Phase 3)
Urinary Bladder Neoplasms (Phase 2/Phase 3)
Urinary Incontinence (Phase 2/Phase 3)
Urination Disorders (Phase 2/Phase 3)
Urological Manifestations (Phase 2)
Vascular Diseases (Phase 4)
Vomiting (Phase 4)
Weight Loss (Early Phase 1)
Wounds and Injuries (Phase 4)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
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