APA-01

APA-01
Clinical data
Other namesAPA01; APA-001; APA001; PharmAla-1; P-1; (R)-2-[(2H-1,3-benzodioxol-5-yl)methyl]pyrrolidine
Drug classEntactogen
ATC code
  • None
Identifiers
  • (2R)-2-(1,3-benzodioxol-5-ylmethyl)pyrrolidine
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC12H15NO2
Molar mass205.257 g·mol−1
3D model (JSmol)
  • C1C[C@@H](NC1)CC2=CC3=C(C=C2)OCO3
  • InChI=1S/C12H15NO2/c1-2-10(13-5-1)6-9-3-4-11-12(7-9)15-8-14-11/h3-4,7,10,13H,1-2,5-6,8H2/t10-/m1/s1
  • Key:IRWQJDYJIAIJSC-SNVBAGLBSA-N

APA-01, also known as PharmAla-1, is an entactogen of the phenethylamine, amphetamine, and MDxx families related to MDMA which is under development for potential medical use. It is a cyclized phenethylamine and is a derivative of MDMA in which the α position has been cyclized with the amine via a propyl group to form a pyrrolidine ring.

The drug is predicted to interact with the monoamine transporters and with the serotonin 5-HT2 receptors. In contrast to MDMA, it does not produce hyperthermia in rodents, instead producing dose-dependent hypothermia. In addition, unlike MDMA, neither APA-01 nor the corresponding (S)- enantiomer showed hyperlocomotion in rodents. Both APA-01 and the (S)- enantiomer produced sympathomimetic cardiovascular effects in rodents, but APA-01 had reduced impact compared to the (S)- enantiomer and relative to MDMA and dextromethamphetamine. APA-01 showed prosocial effects in rodents similarly to MDMA, but with greater potency. The drug is said to have improved safety compared to MDMA.

The chemical synthesis of APA-01 has been described.

APA-01 is under development by PharmAla Biotech. As of April 2026, it is in the preclinical research stage of development. Possible medical applications of APA-01 include treatment of post-traumatic stress disorder (PTSD) and neurological conditions like traumatic brain injury (TBI) and stroke. The drug was first described in the scientific literature, in a conference presentation, by 2024.

See also

References

  1. 1 2 3 "Delving into the Latest Updates on APA-01 with Synapse". Synapse. 8 May 2025. Retrieved 28 April 2026.
  2. 1 2 3 4 5 Kaur H (26 September 2026). APA-01: Development of a Potent Entactogen with Improved Safety Pharmacology Compared to MDMA. European Behavioural Pharmacology Society (EBPS) Biennial Workshop, Banff, Alberta, Canada • 25-27 September 2024 [Novel Pharmacotherapies for Substance Use and Related Mental Health Disorders]. European Behavioural Pharmacology Society (EBPS).
  3. 1 2 3 4 PharmAla Biotech (27 April 2026). "PharmAla Executes Binding Letter of Intent for Formation of Special Purpose Vehicle to Develop Patented Novel MDXX Molecule APA-01". GlobeNewswire News Room (Press release). Retrieved 28 April 2026. [...] APA-01 (also known as PharmAla-1 or "P-1"), the Company's patented novel MDXX molecule. [...] APA-01 is (R)-2-[(2H-1,3-benzodioxol-5-yl)methyl]pyrrolidine, a novel molecule protected by United States Patent No. 12,042,478, with potential therapeutic applications in the treatment of psychological trauma and neurological conditions, including Traumatic Brain Injury and Stroke. APA-01 is part of PharmAla's broader portfolio of novel MDXX class molecules being developed alongside its lead drug candidate, ALA-002, via its Phenesafe.AI drug discovery platform.
  4. 1 2 3 4 5 6 7 8 9 US 12042478, Kaur H, Xin T, "(R)-2-[(2H-1,3-benzodioxol-5-yl)methyl]pyrrolidine and processes for preparation, compositions and uses thereof", published 15 February 2024, issued 23 July 2024, assigned to Pharmala Biotech Pharmala Biotech Inc.