Page last updated: 2024-11-13

gw 1000

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

nabiximols: a combination of the above cpds for treatment of multiple sclerosis pain [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44148067
MeSH IDM0474154

Synonyms (24)

Synonym
tetranabinex
nabidiolex
sativex
56575-23-6
cannador
nabiximols [usan]
unii-k4h93p747o
nabiximols
sab-378
gw-1000-02
tetrahydrocannabinol-cannabidiol combination
cannabidiol and delta-9-tetrahydrocarnabinol
gw1000
sab 378
gw 1000
sab378
delta-9-tetrahydrocannabinol and cannabidiol
gw-1000
k4h93p747o ,
Q891968
DTXSID40972015
5'-methyl-4-pentyl-2'-(prop-1-en-2-yl)-1',2',3',4'-tetrahydro[1,1'-biphenyl]-2,6-diol--6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydro-6h-dibenzo[b,d]pyran-1-ol (1/1)
(6ar,10ar)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydrobenzo[c]chromen-1-ol;2-[(6r)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol
AKOS040753194

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The large majority of adverse effects were mild or moderate, and there were no adverse effect-related withdrawals or serious adverse effects in the active treatment group."( Preliminary assessment of the efficacy, tolerability and safety of a cannabis-based medicine (Sativex) in the treatment of pain caused by rheumatoid arthritis.
Blake, DR; Ho, M; Jubb, RW; McCabe, CS; Robson, P, 2006
)
0.33
" High numbers of subjects experienced at least one adverse event, but most were mild to moderate in severity and all drug-related serious adverse events resolved."( Meta-analysis of the efficacy and safety of Sativex (nabiximols), on spasticity in people with multiple sclerosis.
Collin, C; Duncombe, P; Stott, C; Wade, DT, 2010
)
0.36
" Furthermore, following withdrawal of Sativex, symptoms often return, but, beyond this, sudden cessation is generally safe with no evidence of physiological or psychological dependence."( Evaluation of the safety and tolerability profile of Sativex: is it reassuring enough?
Wade, D, 2012
)
0.38
" The majority of patients (84%) did not report adverse events."( Long-term effectiveness and safety of nabiximols (tetrahydrocannabinol/cannabidiol oromucosal spray) in clinical practice.
Flachenecker, P; Henze, T; Zettl, UK, 2014
)
0.4
" Confusion/ideomotor slowing, fatigue and dizziness were the most frequent side effects; no major adverse events were reported."( Efficacy and safety of nabiximols (Sativex(®)) on multiple sclerosis spasticity in a real-life Italian monocentric study.
Colombo, B; Comi, G; Esposito, F; Ferrè, L; Keller Sarmiento, IJ; Leocani, L; Martinelli Boneschi, F; Martinelli, V; Moiola, L; Nuara, A; Pavan, G; Radaelli, M; Rodegher, M, 2016
)
0.43
" The aim of our study was to describe Sativex effectiveness and adverse events profile in a large population of Italian patients with MS in the daily practice setting."( Efficacy and safety of cannabinoid oromucosal spray for multiple sclerosis spasticity.
Amato, MP; Bergamaschi, R; Bonavita, S; Brescia Morra, V; Bruno Bossio, R; Cavalla, P; Centonze, D; Comi, G; Costantino, GF; Cottone, S; Danni, M; Francia, A; Gajofatto, A; Gasperini, C; Ghezzi, A; Iudice, A; Lus, G; Maniscalco, GT; Marrosu, MG; Matta, M; Messina, S; Mirabella, M; Montanari, E; Patti, F; Pozzilli, C; Rovaris, M; Sessa, E; Solaro, C; Spitaleri, D; Trojano, M; Valentino, P; Zappia, M, 2016
)
0.43
"2%) and/or adverse events (n=268, 18."( Efficacy and safety of cannabinoid oromucosal spray for multiple sclerosis spasticity.
Amato, MP; Bergamaschi, R; Bonavita, S; Brescia Morra, V; Bruno Bossio, R; Cavalla, P; Centonze, D; Comi, G; Costantino, GF; Cottone, S; Danni, M; Francia, A; Gajofatto, A; Gasperini, C; Ghezzi, A; Iudice, A; Lus, G; Maniscalco, GT; Marrosu, MG; Matta, M; Messina, S; Mirabella, M; Montanari, E; Patti, F; Pozzilli, C; Rovaris, M; Sessa, E; Solaro, C; Spitaleri, D; Trojano, M; Valentino, P; Zappia, M, 2016
)
0.43
"Sativex can be a useful and safe option for patients with MS with moderate to severe spasticity resistant to common antispastic drugs."( Efficacy and safety of cannabinoid oromucosal spray for multiple sclerosis spasticity.
Amato, MP; Bergamaschi, R; Bonavita, S; Brescia Morra, V; Bruno Bossio, R; Cavalla, P; Centonze, D; Comi, G; Costantino, GF; Cottone, S; Danni, M; Francia, A; Gajofatto, A; Gasperini, C; Ghezzi, A; Iudice, A; Lus, G; Maniscalco, GT; Marrosu, MG; Matta, M; Messina, S; Mirabella, M; Montanari, E; Patti, F; Pozzilli, C; Rovaris, M; Sessa, E; Solaro, C; Spitaleri, D; Trojano, M; Valentino, P; Zappia, M, 2016
)
0.43
" No serious adverse effects occurred."( Safety and efficacy of nabiximols on spasticity symptoms in patients with motor neuron disease (CANALS): a multicentre, double-blind, randomised, placebo-controlled, phase 2 trial.
Comi, G; Comola, M; Falzone, Y; Fazio, R; Ferraro, OE; Leocani, L; Lunetta, C; Mora, G; Riva, N; Sorarù, G, 2019
)
0.51
" Adverse events were predominantly mild or moderate in severity; however, three cases of hallucinations were reported."( Efficacy and safety of nabiximols cannabinoid medicine for paediatric spasticity in cerebral palsy or traumatic brain injury: a randomized controlled trial.
Checketts, D; Fairhurst, C; Kumar, R; Tayo, B; Turner, S, 2020
)
0.56
"Nabiximols was generally well tolerated; however, neuropsychiatric adverse events were observed."( Efficacy and safety of nabiximols cannabinoid medicine for paediatric spasticity in cerebral palsy or traumatic brain injury: a randomized controlled trial.
Checketts, D; Fairhurst, C; Kumar, R; Tayo, B; Turner, S, 2020
)
0.56
" Aligning with the known safety profile of nabiximols as demonstrated in randomized controlled trials, common adverse events reported consistently across studies conducted under clinical practice conditions were dizziness, fatigue and somnolence."( Safety and tolerability of nabiximols oromucosal spray: a review of real-world experience in observational studies, registries, and case reports.
Prieto González, JM; Vila Silván, C, 2021
)
0.62
" Fewer patients treated with NBX than LAO experienced treatment-related adverse events (25."( Effectiveness, Safety, and Tolerability of Nabiximols Oromucosal Spray vs Typical Oral Long-Acting Opioid Analgesics in Patients with Severe Neuropathic Back Pain: Analysis of 6-Month Real-World Data from the German Pain e-Registry.
Essner, U; Mueller-Schwefe, GHH; Ueberall, MA; Vila Silván, C, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" There are indications that CBD modulates THC's effects, but it is unclear if this is due to a pharmacokinetic and/or pharmacodynamic interaction."( Plasma cannabinoid pharmacokinetics following controlled oral delta9-tetrahydrocannabinol and oromucosal cannabis extract administration.
Darwin, WD; Goodwin, RS; Huestis, MA; Karschner, EL; Wright, S, 2011
)
0.37
"These data suggest that CBD modulation of THC's effects is not due to a pharmacokinetic interaction at these therapeutic doses."( Plasma cannabinoid pharmacokinetics following controlled oral delta9-tetrahydrocannabinol and oromucosal cannabis extract administration.
Darwin, WD; Goodwin, RS; Huestis, MA; Karschner, EL; Wright, S, 2011
)
0.37
"The mean Cmax values (<12 ng/mL) recorded in this study were well below those reported in patients who smoked/inhaled cannabis, which is reassuring since elevated Cmax values are linked to significant psychoactivity."( A phase I study to assess the single and multiple dose pharmacokinetics of THC/CBD oromucosal spray.
Guy, GW; Stott, CG; White, L; Wilbraham, D; Wright, S, 2013
)
0.39
"This review examines the characteristics of nabiximols, its pharmacokinetic properties and data on efficacy and tolerability in MS-related neuropathic pain."( Pharmacokinetic evaluation of nabiximols for the treatment of multiple sclerosis pain.
Constantinescu, CS; Tanasescu, R, 2013
)
0.39
" Study objectives were to evaluate the safety and tolerability of PTL101 containing 10 and 100 mg CBD, following single administrations to healthy volunteers and to compare the pharmacokinetic profiles and relative bioavailability of CBD with Sativex oromucosal spray (the reference product) in a randomized, crossover study design."( Single-Dose Pharmacokinetics of Oral Cannabidiol Following Administration of PTL101: A New Formulation Based on Gelatin Matrix Pellets Technology.
Atsmon, J; Deutsch, F; Deutsch, L; Heffetz, D; Sacks, H, 2018
)
0.48

Compound-Compound Interactions

ExcerptReferenceRelevance
"Nabiximols in combination with MET/CBT was well tolerated and allowed for reduction of cannabis use."( Nabiximols combined with motivational enhancement/cognitive behavioral therapy for the treatment of cannabis dependence: A pilot randomized clinical trial.
Barnes, AJ; Fischer, B; George, TP; Huestis, MA; Le Foll, B; Quilty, LC; Rehm, J; Selby, P; Soliman, A; Staios, G; Streiner, DL; Trigo, JM, 2018
)
0.48

Bioavailability

ExcerptReferenceRelevance
" Relative bioavailability was calculated to determine the relative rate and extent of THC absorption; 5 and 15 mg oral THC bioavailability was 92."( Plasma cannabinoid pharmacokinetics following controlled oral delta9-tetrahydrocannabinol and oromucosal cannabis extract administration.
Darwin, WD; Goodwin, RS; Huestis, MA; Karschner, EL; Wright, S, 2011
)
0.37
" The bioavailability of THC was greater than CBD at single and multiple doses, and there was no evidence of accumulation for any analyte with multiple dosing."( A phase I study to assess the single and multiple dose pharmacokinetics of THC/CBD oromucosal spray.
Guy, GW; Stott, CG; White, L; Wilbraham, D; Wright, S, 2013
)
0.39
"" Lack of standardization, bioavailability issues, and ultimately prohibition were all factors in cannabis-based medicines failing to maintain mainstream usage in seizure treatment, but investigation was resumed in the 1970s with interesting signals noted in both laboratory and clinical settings."( Cannabis and epilepsy: An ancient treatment returns to the fore.
Russo, EB, 2017
)
0.46
" Study objectives were to evaluate the safety and tolerability of PTL101 containing 10 and 100 mg CBD, following single administrations to healthy volunteers and to compare the pharmacokinetic profiles and relative bioavailability of CBD with Sativex oromucosal spray (the reference product) in a randomized, crossover study design."( Single-Dose Pharmacokinetics of Oral Cannabidiol Following Administration of PTL101: A New Formulation Based on Gelatin Matrix Pellets Technology.
Atsmon, J; Deutsch, F; Deutsch, L; Heffetz, D; Sacks, H, 2018
)
0.48
" The oral bioavailability of THC and CBD is very low due to extensive "first-pass" metabolism."( PTL401, a New Formulation Based on Pro-Nano Dispersion Technology, Improves Oral Cannabinoids Bioavailability in Healthy Volunteers.
Atsmon, J; Cherniakov, I; Deutsch, F; Deutsch, L; Domb, AJ; Heffetz, D; Hoffman, A; Izgelov, D; Sacks, H, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" Sativex is a sublingual spray on Cannabis extract basis, and is equipped with an electronic tool to facilitate accurate dosing and to prevent misuses."( [A novel analgesics made from Cannabis].
Szendrei, K, 2004
)
0.32
" Patients self titrate their overall dose and pattern of dosing according to their response to and tolerance of the medicine."( Sativex: clinical efficacy and tolerability in the treatment of symptoms of multiple sclerosis and neuropathic pain.
Barnes, MP, 2006
)
0.33
" No tolerance to the benefit of Sativex on pain or sleep, nor need for dosage increases have been noted in safety extension studies of up to four years, wherein 40-50% of subjects attained good or very good sleep quality, a key source of disability in chronic pain syndromes that may contribute to patients' quality of life."( Cannabis, pain, and sleep: lessons from therapeutic clinical trials of Sativex, a cannabis-based medicine.
Guy, GW; Robson, PJ; Russo, EB, 2007
)
0.34
"Nine cannabis smokers completed all 5 dosing sessions."( Plasma cannabinoid pharmacokinetics following controlled oral delta9-tetrahydrocannabinol and oromucosal cannabis extract administration.
Darwin, WD; Goodwin, RS; Huestis, MA; Karschner, EL; Wright, S, 2011
)
0.37
" In an experimental mouse model of MS-related spasticity, Sativex dose-dependently improved hind limb flexion/stiffness and a dosage of 10 mg/kg was shown to be as effective as the most widely established anti-spasticity treatment baclofen (5 mg/kg)."( Endocannabinoid pathways and their role in multiple sclerosis-related muscular dysfunction.
Di Marzo, V, 2011
)
0.37
" Secondary outcomes were to determine evidence of developing tolerance and to assess the long-term dosing profile of Sativex."( Sativex long-term use: an open-label trial in patients with spasticity due to multiple sclerosis.
Collin, C; Notcutt, W; Serpell, MG, 2013
)
0.39
"5 h after dosing and analyzed for THC, CBD, cannabinol (CBN), and 11-nor-9-carboxy-THC (THCCOOH)."( Can oral fluid cannabinoid testing monitor medication compliance and/or cannabis smoking during oral THC and oromucosal Sativex administration?
Barnes, AJ; Goodwin, RS; Huestis, MA; Karschner, EL; Lee, D; Milman, G, 2013
)
0.39
" THCCOOH/THC ratios increased throughout each dosing session."( Can oral fluid cannabinoid testing monitor medication compliance and/or cannabis smoking during oral THC and oromucosal Sativex administration?
Barnes, AJ; Goodwin, RS; Huestis, MA; Karschner, EL; Lee, D; Milman, G, 2013
)
0.39
" There was evidence of dose-proportionality in the single but not the multiple dosing data sets."( A phase I study to assess the single and multiple dose pharmacokinetics of THC/CBD oromucosal spray.
Guy, GW; Stott, CG; White, L; Wilbraham, D; Wright, S, 2013
)
0.39
"Neuropathic pain caused by chemotherapy limits dosing and duration of potentially life-saving anti-cancer treatment and impairs quality of life."( A double-blind, placebo-controlled, crossover pilot trial with extension using an oral mucosal cannabinoid extract for treatment of chemotherapy-induced neuropathic pain.
Cesar-Rittenberg, P; Hohmann, AG; Lynch, ME, 2014
)
0.4
" Oral fluid was tested prior to and immediately after dosing with either Sativex(®) or placebo at intervals up to 2h after the dose."( The detection of THC, CBD and CBN in the oral fluid of Sativex® patients using two on-site screening tests and LC-MS/MS.
Allsop, DJ; Copeland, J; Fu, S; Lewis, J; Molnar, A, 2014
)
0.4
" Meaningful symptomatic improvement was achieved within the recommended dosage limit of ≤12 sprays per day."( Effect of Sativex on spasticity-associated symptoms in patients with multiple sclerosis.
Dechant, KL; Meuth, SG; Vila, C, 2015
)
0.42
" Open-label studies performed to date with a focus on effectiveness have indicated that about one-half to two-thirds of patients initiated on THC:CBD oromucosal spray continue to derive benefit after 3 months' treatment at a mean dosage of 5-7 sprays/day."( Advances in the management of MS symptoms: real-life evidence.
Trojano, M, 2015
)
0.42
" Stretch reflex responders were taking a significantly higher number of puffs, whereas no differences were found in the responders by the other scales, suggesting that a higher dosage would add benefit if tolerated."( The effect of cannabinoids on the stretch reflex in multiple sclerosis spasticity.
Abbruzzese, G; Bandini, F; Canneva, S; Capello, E; Colombano, F; Currà, A; Fattapposta, F; Marinelli, L; Mori, L; Trompetto, C, 2016
)
0.43
" No significant symptomatic effects were detected at the prescribed dosage and for a 12-week period."( A double-blind, randomized, cross-over, placebo-controlled, pilot trial with Sativex in Huntington's disease.
Alonso Arias, MA; Fernández Ruiz, J; Galve-Roperh, I; García Caldentey, J; García de Yébenes Prous, J; García de Yébenes, MJ; García Ribas, G; García-Bermejo, ML; Guzmán, M; López-Sendón Moreno, JL; Ortega-Gutierrez, S; Resel, E; Ruiz Romero, C; Sagredo, O; Tolón, RM; Trigo Cubillo, P; Valdeolivas, S, 2016
)
0.43
"Sativex was well-tolerated by all participants (average dosage 77."( Sativex Associated With Behavioral-Relapse Prevention Strategy as Treatment for Cannabis Dependence: A Case Series.
Barnes, AJ; Fischer, B; George, TP; Huestis, MA; Le Foll, B; Quilty, L; Rehm, J; Selby, P; Soliman, A; Staios, G; Trigo, JM,
)
0.13
" THC:CBD mean dosage was 6 sprays/day."( Tetrahydrocannabinol:Cannabidiol Oromucosal Spray for Multiple Sclerosis-Related Resistant Spasticity in Daily Practice.
Trojano, M; Vermersch, P, 2016
)
0.43
" We lack valid data on the safety, efficacy, and dosing of artisanal preparations available from dispensaries in the 25 states and District of Columbia with MMJ programs and online sources of CBD and other cannabinoids."( Cannabinoids in treatment-resistant epilepsy: A review.
Devinsky, O; Gloss, D; O'Connell, BK, 2017
)
0.46
", methods of administration (smoking, vaporisation, oral), and dosing recommendations."( Practical considerations in medical cannabis administration and dosing.
MacCallum, CA; Russo, EB, 2018
)
0.48
" This paper provides an overview of the available cannabinoid-based formulations, a summary of the highest quality evidence for the use of cannabinoids for treating spasticity and pain associated with multiple sclerosis (MS), and a discussion of possible dosing regimens based on information from these studies."( Cannabinoids for Treatment of MS Symptoms: State of the Evidence.
Cameron, M; Rice, J, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (226)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's20 (8.85)29.6817
2010's157 (69.47)24.3611
2020's49 (21.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.42

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.42 (24.57)
Research Supply Index5.62 (2.92)
Research Growth Index5.42 (4.65)
Search Engine Demand Index81.58 (26.88)
Search Engine Supply Index3.93 (0.95)

This Compound (31.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials49 (21.59%)5.53%
Reviews66 (29.07%)6.00%
Case Studies10 (4.41%)4.05%
Observational17 (7.49%)0.25%
Other85 (37.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]