R13 (drug)

Last updated
R13
R13.svg
Clinical data
Other namesR-13; BrAD-R13; BrADR13; Braegen-01; Braegen01; 4-Oxo-2-phenyl-4H-chromene-7,8-diyl bis(methylcarbamate)
Routes of
administration 		Oral [1] [2]
Drug class TrkB agonist
ATC code
  • None
Pharmacokinetic data
Metabolites Tropoflavin [2]
Identifiers
  • [8-(methylcarbamoyloxy)-4-oxo-2-phenylchromen-7-yl] N-methylcarbamate
CAS Number
PubChem CID
UNII
Chemical and physical data
Formula C19H16N2O6
Molar mass 368.345 g·mol−1
3D model (JSmol)
  • CNC(=O)OC1=C(C2=C(C=C1)C(=O)C=C(O2)C3=CC=CC=C3)OC(=O)NC
  • InChI=1S/C19H16N2O6/c1-20-18(23)26-14-9-8-12-13(22)10-15(11-6-4-3-5-7-11)25-16(12)17(14)27-19(24)21-2/h3-10H,1-2H3,(H,20,23)(H,21,24)
  • Key:NWWRHMSYZTWUBD-UHFFFAOYSA-N

R13, also known as BrAD-R13 or as Braegen-01, is a small-molecule flavonoid and orally active, potent, and selective agonist of the tropomyosin receptor kinase B (TrkB), the main signaling receptor for the neurotrophin brain-derived neurotrophic factor (BDNF), which is under development for the potential treatment of Alzheimer's disease, amyotrophic lateral sclerosis (ALS), depressive disorders, Parkinson's disease, and schizophrenia. [1] [3] [4] [5] [2] [6] [7] It is taken orally. [1]

Contents

The drug is a structural modification and prodrug of 7,8-dihydroxyflavone (7,8-DHF; tropoflavin) with improved potency and pharmacokinetics, namely oral bioavailability and duration. [4] [5] [2] The compound is a replacement for the earlier tropoflavin prodrug R7 and has similar properties to it. [2] [8] It was developed because while R7 displayed a good drug profile in animal studies, it showed almost no conversion into tropoflavin in human liver microsomes. [2] In contrast to R7, R13 is readily hydrolyzed into tropoflavin in human liver microsomes. [2]

R13, under the synonym and developmental code name BrAD-R13, is being developed by Braegen Pharmaceutical in China. [1] [3] [7] As of August 2025, it is in phase 1 clinical trials for Alzheimer's disease and the preclinical research stage of development for all other indications. [1] [3]

See also

References

  1. 1 2 3 4 5 "BrAD R13". AdisInsight. 8 August 2025. Retrieved 24 January 2026.
  2. 1 2 3 4 5 6 7 Chen C, Wang Z, Zhang Z, Liu X, Kang SS, Zhang Y, Ye K (January 2018). "The prodrug of 7,8-dihydroxyflavone development and therapeutic efficacy for treating Alzheimer's disease". Proc. Natl. Acad. Sci. U.S.A. 115 (3): 578–583. Bibcode:2018PNAS..115..578C. doi: 10.1073/pnas.1718683115 . PMC   5777001 . PMID   29295929.
  3. 1 2 3 "Delving into the Latest Updates on BrAD-R13 with Synapse". Synapse. 20 December 2025. Retrieved 24 January 2026.
  4. 1 2 Liu W, Wang X, O'Connor M, Wang G, Han F (2020). "Brain-Derived Neurotrophic Factor and Its Potential Therapeutic Role in Stroke Comorbidities". Neural Plasticity. 2020 1969482. doi: 10.1155/2020/1969482 . PMC   7204205 . PMID   32399020. Recently, a derivative of 7,8-DHF, namely, BrAD-R13, was approved by the FDA for use in clinical trials for the treatment of mild to moderate AD.
  5. 1 2 Wang D, Lang ZC, Wei SN, Wang W, Zhang H (June 2024). "Targeting brain-derived neurotrophic factor in the treatment of neurodegenerative diseases: A review". Neuroprotection. 2 (2): 67–78. doi:10.1002/nep3.43. PMC   12486910 . PMID   41383700. BrAD‐R13, a derivative of 7,8‐ DHF, has been approved by the FDA for clinical trials in mild to moderate disease, with preclinical studies supporting its efficacy against AD and ALS.18,134–136 Recently, BrAD‐R13 has been registered for a Phase I trial in China (CTR20233658).
  6. ↑ USapplication 20150274692,Keqiang Ye,"7,8-Dihydoxyflavone and 7,8-substituted flavone derivatives, compositions, and methods related thereto",published 2015-10-01, assigned to Emory University
  7. 1 2 "Crystal form B of 7, 8-dihydroxyflavone derivative, and preparation method and application thereof". Google Patents. 20 August 2020. Retrieved 9 February 2026. Chinese patent application CN201380062367.X discloses that 7,8-dihydroxy flavone is modified to obtain 7,8-dihydroxy flavone derivatives with structural formula [chemical structure, I] (abbreviated as compound of formula I or compound BrAD-R13). In-vivo non-clinical tests show that the compound of the formula I has the half-life and the bioavailability which are obviously improved compared with 7,8-DHF, and has stronger drug property.
  8. ↑ Liu C, Chan CB, Ye K (2016). "7,8-dihydroxyflavone, a small molecular TrkB agonist, is useful for treating various BDNF-implicated human disorders". Transl Neurodegener. 5 2. doi: 10.1186/s40035-015-0048-7 . PMC   4702337 . PMID   26740873.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.