Overview
Nabilone (marketed as Cesamet) is a synthetic form of delta-9-tetrahydrocannabinol (Δ⁹-THC), the primary psychoactive component of cannabis (marijuana). Although structurally distinct from THC, nabilone mimics THC's structure and pharmacological activity through weak partial agonist activity at Cannabinoid-1 (CB1R) and Cannabinoid-2 (CB2R) receptors, however it is considered to be twice as active as Δ⁹-THC. Nabilone is approved by the FDA for the treatment of nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetic treatments . Tetrahydrocannabinol (THC) and cannabidiol (CBD) are the two most abundant cannabinoids found naturally in the resin of the marijuana plant, both of which are pharmacologically active due to their interaction with cannabinoid receptors that are found throughout the body . While both CBD and THC are used for medicinal purposes, they have different receptor activity, function, and physiological effects. If not provided in their activated form (such as through synthetic forms like Nabilone or Dronabinol), THC and CBD are obtained through conversion from their precursors, tetrahydrocannabinolic acid-A (THCA-A) and cannabidiolic acid (CBDA), through decarboxylation reactions. This can be achieved through heating, smoking, vaporization, or baking of dried unfertilized female cannabis flowers. From a pharmacological perspective, Cannabis' diverse receptor profile explains its potential application for such a wide variety of medical conditions. Cannabis contains more than 400 different chemical compounds, of which 61 are considered cannabinoids, a class of compounds that act upon endogenous cannabinoid receptors of the body . The endocannabinoid system is widely distributed throughout the central and peripheral nervous system (via the Cannabinoid Receptors CB1 and CB2) and plays a role in many physiological processes such as inflammation, cardiovascular function, learning, pain, memory, stress and emotional regulation, and the sleep/wake cycle among many others . CB1 receptors are found in both the central and peripheral nervous system, and are most abundant in the hippocampus and amygdala, which are the areas of the brain responsible for short-term memory storage and emotional regulation. CB2 receptors are mainly located in the peripheral nervous system and can be found on lymphoid tissue where they are involved in regulation of immune function . In Canada, the United States, the United Kingdom and Mexico, nabilone is marketed as Cesamet. It was approved in 1985 by the United States FDA for treatment of chemotherapy-induced nausea and vomiting that has not responded to conventional antiemetics. Though it was approved by the FDA in 1985, the drug only began marketing in the United States in 2006. It is also approved for use in treatment of anorexia and weight loss in patients with AIDS. Nabilone is a racemate consisting of the (S,S) and the (R,R) isomers.
Indication
Nabilone is indicated for the treatment of the nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetic treatments. This restriction is required because a substantial proportion of any group of patients treated with Nabilone can be expected to experience disturbing psychotomimetic reactions not observed with other antiemetic agents.
Associated Conditions
- Refractory Chemotherapy-Induced Nausea and Vomiting (CINV)
Research Report
Nabilone (DB00486): A Comprehensive Pharmacological and Clinical Monograph
1.0 Executive Summary
Nabilone is an orally active, synthetic cannabinoid and a structural analog of delta-9-tetrahydrocannabinol (Δ⁹-THC), the principal psychoactive constituent of cannabis. Identified by DrugBank ID DB00486 and CAS Number 51022-71-0, Nabilone functions as a partial agonist at both cannabinoid type 1 (CB1) and type 2 (CB2) receptors within the body's endocannabinoid system. Its therapeutic effects, particularly its antiemetic properties, are primarily mediated through its action on CB1 receptors in the central nervous system.
The United States Food and Drug Administration (FDA) has approved Nabilone for a narrow indication: the treatment of nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond adequately to conventional antiemetic therapies. This positions Nabilone as a second-line or salvage agent in oncology support. Despite this limited approval, the drug is subject to extensive off-label use and investigation for a range of intractable conditions, including chronic non-cancer pain, fibromyalgia, spasticity-related pain in neurological disorders, and the suppression of nightmares associated with post-traumatic stress disorder (PTSD).
The clinical utility of Nabilone is fundamentally defined by a delicate balance between its potential therapeutic benefits and a prominent profile of adverse effects. Its safety and tolerability are dominated by dose-limiting central nervous system effects, including drowsiness, vertigo, euphoria, and potential psychiatric disturbances such as hallucinations and psychosis, which can persist for up to 72 hours after administration. Due to its psychoactive properties and potential for psychological dependence, Nabilone is classified as a Schedule II controlled substance in the United States and Canada, necessitating stringent prescribing and monitoring protocols.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2023/06/02 | Phase 4 | Recruiting | |||
2023/02/24 | Phase 2 | Recruiting | Simon Ducharme, MD | ||
2022/08/10 | Phase 2 | Completed | PleoPharma, Inc. | ||
2022/03/10 | Phase 1 | Recruiting | Hsiang-Yuan Lin | ||
2022/01/06 | Phase 3 | Completed | |||
2021/05/10 | Phase 1 | Withdrawn | |||
2021/03/19 | Phase 2 | Withdrawn | |||
2021/03/17 | Phase 2 | Terminated | |||
2020/08/17 | Phase 3 | Recruiting | |||
2019/08/15 | Phase 3 | Completed | Eldon Loh, MD |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Bausch Health US LLC | 0187-1231 | ORAL | 1 mg in 1 1 | 1/19/2021 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| PMS-NABILONE | 02380900 | Capsule - Oral | 0.5 MG | 3/26/2012 | |
| TEVA-NABILONE | teva canada limited | 02384884 | Capsule - Oral | 0.5 MG | 5/23/2012 |
| PMS-NABILONE | 02380897 | Capsule - Oral | 0.25 MG | 1/22/2021 | |
| CESAMET | bausch health, canada inc. | 02256193 | Capsule - Oral | 0.5 MG | 9/16/2004 |
| APO-NABILONE | 02441497 | Capsule - Oral | 0.25 MG | N/A | |
| ACT NABILONE | teva canada limited | 02393603 | Capsule - Oral | 1 MG | 10/2/2012 |
| CESAMET | bausch health, canada inc. | 02312263 | Capsule - Oral | 0.25 MG | 9/12/2008 |
| TEVA-NABILONE | teva canada limited | 02392925 | Capsule - Oral | 0.25 MG | 5/27/2013 |
| APO-NABILONE | 02441519 | Capsule - Oral | 1 MG | N/A | |
| PMS-NABILONE | 02380919 | Capsule - Oral | 1.0 MG | 3/26/2012 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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