ASP-3652
A peripheral FAAH inhibitor (Astellas), with no efficacy demonstrated in phase 2.
Harm-reduction warning
No characterised human dose: animal / in vitro data only. Effect profile, safety margin and acute toxicity are not documented in human clinical practice. Extremely potent compound: severe effects, seizures and deaths reported in the literature.
C₂₇H₃₂N₂O₄S₂
CID 11352782
- Family
- ECS pharmacological toolEnzyme inhibitor
- Molar mass
- 512.70 g/mol
Updated on
In plain terms
ASP-3652 is a laboratory molecule developed by the pharmaceutical group Astellas. It does not exist in hemp: rather than imitating cannabis, it slows the enzyme that destroys the cannabinoids the body makes itself. Tested in people with prostate and pelvic pain, then bladder pain, it did no better than a placebo on pain and was never put on sale.
Receptors and activity
Target network
- Blocks or inhibits
The lower the cited value, the closer the target sits to ASP-3652: one ring per factor of 100. A target with no measured value stays on the edge.
Where these targets live
Where each target has been found in humans, according to the cited studies. The map shows the target, not an effect of ASP-3652.
FAAHFAAH found in 7 regions of the body
- CortexpresentCortical pyramidal neurons1
- Basal gangliapresentStriatal neurons1
- HypothalamuspresentPresent in hypothalamic nuclei1
- CerebellumpresentPurkinje cells and cerebellar layers1
- BrainstempresentInferior olivary nuclei1
- Adipose tissuepresentExpressed in mature adipocytes2
- BonepresentPresent on osteoclasts3
Map sources
- Romero J et al. Fatty acid amide hydrolase localization in the human central nervous system: an immunohistochemical study. Brain Res Mol Brain Res, 2002 (new tab)
- Engeli S et al. Activation of the peripheral endocannabinoid system in human obesity. Diabetes, 2005 (new tab)
- Rossi F et al. The endovanilloid/endocannabinoid system in human osteoclasts: possible involvement in bone formation and resorption. Bone, 2009 (new tab)
Cited values
- FAAHInhibitorno measured value cited
Pharmacology
ASP-3652 is a reversible inhibitor of FAAH, the enzyme that hydrolyses anandamide and neighbouring N-acylethanolamines. It does not itself bind CB1 or CB2: by slowing degradation, it raises plasma concentrations of anandamide, oleoylethanolamide and palmitoylethanolamide. The molecule is described as peripherally acting, and the human data point the same way: after repeated doses, the area under the curve in cerebrospinal fluid was about 0.2% of that in plasma, with no central adverse effect even at supratherapeutic doses (Takizawa et al. 2020). Phase 1 trials showed dose-dependent inhibition of FAAH and a rise in plasma endocannabinoids, but the two published phase 2 trials showed no efficacy: in men with chronic prostatitis or chronic pelvic pain syndrome, the study was stopped for futility at the interim analysis (239 patients randomised; Wagenlehner et al. 2017), and in 287 women with interstitial cystitis, the highest dose, 300 mg twice a day, differed from placebo by 0.02 points on mean daily pain (Houbiers et al. 2021). No therapeutic benefit is established.
Key sources.
- Takizawa M et al., Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP3652 in First-in-Human Studies, Adv Ther, 2020 (new tab)PMID 32681461
- Takizawa M et al., Investigation of Safety and Tolerability of ASP3652 Based on Clinical Studies, including cerebrospinal fluid penetration, Adv Ther, 2020 (new tab)PMID 32715381
- Takizawa M et al., Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ASP3652, a Reversible Fatty Acid Amide Hydrolase Inhibitor, Clin Ther, 2020 (new tab)PMID 32456804
- Wagenlehner FME et al., Fatty Acid Amide Hydrolase Inhibitor Treatment in Men With Chronic Prostatitis, Chronic Pelvic Pain Syndrome, Urology, 2017 (new tab)PMID 28254462
- Houbiers JGA et al., An adaptive randomized clinical trial in interstitial cystitis, bladder pain syndrome evaluating efficacy of ASP3652, World J Urol, 2021 (new tab)PMID 32734461
- The endocannabinoid system, current implications for drug development, J Intern Med, 2021 (review of the FAAH inhibitor class, including the BIA 10-2474 incident) (new tab)PMID 33348434
- PubChem, CID 11352782, identifiers and synonyms (new tab)
- ClinicalTrials.gov, NCT01613586, phase 2 trial of ASP3652 in interstitial cystitis, sponsor Astellas Pharma Europe (new tab)
History
- Source
- An entirely synthetic molecule, born of industrial medicinal chemistry. It is produced neither by hemp nor by any other plant, and has never been identified in a natural product. Its only documented existence is that of an experimental drug candidate, never marketed.
Origin
Research tool
No natural biosynthetic pathway: this molecule falls exclusively within chemical synthesis and is not a plant metabolite. Its action, by contrast, bears on endocannabinoid metabolism, since it blocks the hydrolysis of anandamide, which is made on demand by cell membranes and then normally destroyed by FAAH.
Legal framework
- European Union
An investigational medicine, studied in clinical trials; no marketing authorisation.
- France
Not classified: absent from the ANSM list of narcotics (consolidated version updated 16/02/2026), and its structure (a biphenyl acylsulfonamide) falls within no generic family of Annex IV. An investigational medicine, with no marketing authorisation.
Sources: EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA. Our method.
Classification
Family, origin and source verification
- Family
ECS pharmacological tool › Enzyme inhibitor
- Verification
Classification, sources and binding values checked on 20 October 2026; text read against its sources and Wikipedia.
- Wikipedia (English)
No dedicated article.
References
- Takizawa M et al., Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP3652 in First-in-Human Studies, Adv Ther, 2020 (new tab)PMID 32681461
- Takizawa M et al., Investigation of Safety and Tolerability of ASP3652 Based on Clinical Studies, including cerebrospinal fluid penetration, Adv Ther, 2020 (new tab)PMID 32715381
- Takizawa M et al., Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ASP3652, a Reversible Fatty Acid Amide Hydrolase Inhibitor, Clin Ther, 2020 (new tab)PMID 32456804
- Wagenlehner FME et al., Fatty Acid Amide Hydrolase Inhibitor Treatment in Men With Chronic Prostatitis, Chronic Pelvic Pain Syndrome, Urology, 2017 (new tab)PMID 28254462
- Houbiers JGA et al., An adaptive randomized clinical trial in interstitial cystitis, bladder pain syndrome evaluating efficacy of ASP3652, World J Urol, 2021 (new tab)PMID 32734461
- The endocannabinoid system, current implications for drug development, J Intern Med, 2021 (review of the FAAH inhibitor class, including the BIA 10-2474 incident) (new tab)PMID 33348434
- PubChem, CID 11352782, identifiers and synonyms (new tab)
- ClinicalTrials.gov, NCT01613586, phase 2 trial of ASP3652 in interstitial cystitis, sponsor Astellas Pharma Europe (new tab)
Identifiers
Names
- IUPAC name
- 4-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]-N-methylsulfonyl-2-propan-2-ylsulfanylbenzamide
- Other names
- ASP3652
Identifiers
- Formula
- C₂₇H₃₂N₂O₄S₂
- PubChem CID
- 11352782(new tab)
- InChIKey
- HXFKZSVPCHUKBX-VWLOTQADSA-N
- SMILES
- CC(C)
SC1= C(C= CC(= C1) C2= CC= C(C= C2) CCNC[C@@H] (C3= CC= CC= C3) O) C(= O) NS(= O) (= O) C
LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.