IMAGABALIN

Imagabalin
Clinical data
Other names	PD-0332334; PD-332,334
ATC code	None;
Identifiers
	IUPAC name (3S,5R)-3-amino-5-methyloctanoic acid;
CAS Number	610300-07-7 ; 610300-00-0 ( hydrochloride);
PubChem CID	10236037;
ChemSpider	8411525;
UNII	NDG6931B7H;
KEGG	D09627;
CompTox Dashboard ( EPA)	DTXSID00976534 ;
Chemical and physical data
Formula	C9H19NO2
Molar mass	173.256 g·mol−1
3D model ( JSmol)	Interactive image;
	SMILES O=C(O)C[C@@H](N)C[C@@H](CCC)C;
	InChI InChI=1S/C9H19NO2/c1-3-4-7(2)5-8(10)6-9(11)12/h7-8H,3-6,10H2,1-2H3,(H,11,12)/t7-,8+/m1/s1; Key:JXEHXYFSIOYTAH-SFYZADRCSA-N;

Imagabalin ( INN, USAN; PD-0332334) was an investigational drug that acts as a ligand for the α₂δ subunit of the voltage-dependent calcium channel,^[1] with some selectivity for the α₂δ₁ subunit over α₂δ₂.^[2] It was under development by Pfizer as a pharmaceutical medication due to its hypothesized anxiolytic, analgesic, hypnotic, and anticonvulsant-like activity. It reached phase-III clinical trials for treatment of generalized anxiety disorder; however, the trials were terminated by the manufacturer.^[3]^[4]^[5]^[6] The drug is no longer under development.

References

^ Quintero JE, Pomerleau F, Huettl P, Johnson KW, Offord J, Gerhardt GA (July 2011). "Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology". Brain Research. 1401: 1–9. doi: 10.1016/j.brainres.2011.05.025. PMC 3197737. PMID 21664606.
^ Larry Ereshefsky (2008). "Therapies in the Pipeline for Sleep Disorders: Focus on Novel Mechanisms and Disease Models" (PDF) (Press release). p. 11. Retrieved 2012-04-22.
^ Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study Of PD 0332334 And Paroxetine Evaluating The Efficacy And Safety Of PD 0332334 For The Treatment Of Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)
^ Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study Of PD 0332334 And Paroxetine Evaluating The Efficacy And Safety Of PD 0332334 For The Treatment Of Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)
^ Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study of PD 0332334 and Paroxetine Evaluating the Efficacy and Safety of PD 0332334 for the Treatment of Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)
^ Pfizer (2012-11-09). "A 52-Week Open-Label Safety Study of PD 0332334 in Subjects With Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)

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[pmid21664606-1] Quintero JE, Pomerleau F, Huettl P, Johnson KW, Offord J, Gerhardt GA (July 2011). "Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology". Brain Research. 1401: 1–9. doi: 10.1016/j.brainres.2011.05.025. PMC 3197737. PMID 21664606.

[Ereshefsky2008-2] Larry Ereshefsky (2008). "Therapies in the Pipeline for Sleep Disorders: Focus on Novel Mechanisms and Disease Models" (PDF) (Press release). p. 11. Retrieved 2012-04-22.

[3] Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study Of PD 0332334 And Paroxetine Evaluating The Efficacy And Safety Of PD 0332334 For The Treatment Of Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)

[4] Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study Of PD 0332334 And Paroxetine Evaluating The Efficacy And Safety Of PD 0332334 For The Treatment Of Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)

[5] Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study of PD 0332334 and Paroxetine Evaluating the Efficacy and Safety of PD 0332334 for the Treatment of Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)

[6] Pfizer (2012-11-09). "A 52-Week Open-Label Safety Study of PD 0332334 in Subjects With Generalized Anxiety Disorder". {{ cite journal}}: Cite journal requires |journal= ( help)

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v t e Anxiolytics ( N05B)
5-HT_1ARTooltip 5-HT1A receptor agonists	Buspirone Gepirone Tandospirone
GABA_ARTooltip GABAA receptor PAMsTooltip positive allosteric modulators	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam; Others: Alpidem^‡ Barbiturates (e.g., phenobarbital) Carbamates (e.g., meprobamate) Carisoprodol Chlormezanone^‡ Ethanol (alcohol) Etifoxine
Hypnotics	Zopiclone
Gabapentinoids ( α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., escitalopram) SNRIsTooltip Serotonin-norepinephrine reuptake inhibitors (e.g., duloxetine) SARIsTooltip Serotonin antagonist and reuptake inhibitors (e.g., trazodone) TCAsTooltip Tricyclic antidepressants (e.g., clomipramine^#) TeCAsTooltip Tetracyclic antidepressants (e.g., mirtazapine) MAOIsTooltip Monoamine oxidase inhibitors (e.g., phenelzine); Others: Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Antipsychotics	Quetiapine Flupentixol
Sympatholytics ( Antiadrenergics)	Alpha-1 blockers (e.g., prazosin) Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) Beta blockers (e.g., propranolol)
Others	Benzoctamine Cycloserine Fabomotizole Hydroxyzine Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^# WHO-EM ^‡ Withdrawn from market Clinical trials: ^† Phase III ^§Never to phase III

v t e Anxiolytics ( N05B)
5-HT_1ARTooltip 5-HT1A receptor agonists	Buspirone Gepirone Tandospirone
GABA_ARTooltip GABAA receptor PAMsTooltip positive allosteric modulators	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam; Others: Alpidem^‡ Barbiturates (e.g., phenobarbital) Carbamates (e.g., meprobamate) Carisoprodol Chlormezanone^‡ Ethanol (alcohol) Etifoxine
Hypnotics	Zopiclone
Gabapentinoids ( α₂δ VDCC blockers)	Gabapentin Gabapentin enacarbil Phenibut Pregabalin
Antidepressants	SSRIsTooltip Selective serotonin reuptake inhibitors (e.g., escitalopram) SNRIsTooltip Serotonin-norepinephrine reuptake inhibitors (e.g., duloxetine) SARIsTooltip Serotonin antagonist and reuptake inhibitors (e.g., trazodone) TCAsTooltip Tricyclic antidepressants (e.g., clomipramine^#) TeCAsTooltip Tetracyclic antidepressants (e.g., mirtazapine) MAOIsTooltip Monoamine oxidase inhibitors (e.g., phenelzine); Others: Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine
Antipsychotics	Quetiapine Flupentixol
Sympatholytics ( Antiadrenergics)	Alpha-1 blockers (e.g., prazosin) Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) Beta blockers (e.g., propranolol)
Others	Benzoctamine Cycloserine Fabomotizole Hydroxyzine Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum
^# WHO-EM ^‡ Withdrawn from market Clinical trials: ^† Phase III ^§Never to phase III

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