Balumorexton

Balumorexton
Clinical data
Other namesTAK-360; TAK360
Routes of
administration		Oral[1]
Drug classOrexin OX2 receptor antagonist; Wakefulness-promoting agent
Identifiers
  • N-[(6R)-7,7-difluoro-2-[5-fluoro-4-(2,4,6-trifluorophenyl)-1,2-benzoxazol-3-yl]-3-oxo-5,6-dihydropyrrolo[1,2-c]imidazol-6-yl]methanesulfonamide
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC20H12F6N4O4S
Molar mass518.39 g·mol−1
3D model (JSmol)
  • CS(=O)(=O)N[C@@H]1CN2C(=CN(C2=O)C3=NOC4=C3C(=C(C=C4)F)C5=C(C=C(C=C5F)F)F)C1(F)F
  • InChI=1S/C20H12F6N4O4S/c1-35(32,33)28-13-6-29-14(20(13,25)26)7-30(19(29)31)18-17-12(34-27-18)3-2-9(22)16(17)15-10(23)4-8(21)5-11(15)24/h2-5,7,13,28H,6H2,1H3/t13-/m1/s1
  • Key:QYIMOBVUEGPQSO-CYBMUJFWSA-N

Balumorexton (INNTooltip International Nonproprietary Name; likely developmental code name TAK-360) is a selective orexin OX2 receptor agonist which is under development for the treatment of narcolepsy and idiopathic hypersomnia.[1][2][3][4][5][6] It is taken orally.[1] The drug is under development by Takeda.[1] As of June 2025, it is in phase 2 clinical trials for both narcolepsy and idiopathic hypersomnia.[1]

See also

References

  1. ^ a b c d e "TAK 360". AdisInsight. 8 June 2025. Retrieved 5 June 2026.
  2. ^ "Delving into the Latest Updates on TAK-360 with Synapse". Synapse. 4 June 2026. Retrieved 5 June 2026.
  3. ^ "WHO2026" (PDF). cdn.who.int.
  4. ^ "balumorexton". IUPHAR/BPS Guide to PHARMACOLOGY. Retrieved 5 June 2026. balumorexton: Synonyms: example 77 [WO2024095133]. [...] Comment: The chemical structure for balumorexton was obtained from WHO INN proposed list 134 (Feb 2026), in which it is described as an orexin receptor agonist and potential narcolepsy therapeutic. The structure is claimed in Takeda patent WO2024095133 [1]. At time of curation (Feb 2026) Takeda's declared development pipeline contained two OX2 receptor agonists, oveporexton (TAK-861) and TAK-360, so balumorexton is likely the INN for the latter candidate. Balumorexton is a benzisoxazole-containing compound.
  5. ^ "The Swiss Army Knife of Heterocycles: Isoxazoles Across Drug Discovery". Drug Hunter. 9 March 2026. Retrieved 5 June 2026. Balumorexton is a novel benzisoxazole-containing OX2R agonist, that our research indicates is likely to correspond to Takeda's pipeline compound TAK-360. Assuming a similar binding mode to oveporexton, that involves an interaction between the sulfonamide motif and Gln134, the introduction of the benzisoxazole in balumorexton could provide conformational control of the biaryl motif.
  6. ^ Morse AM (May 2025). "Enhancing the Management of Hypersomnia: Examining the Role of the Orexin System". Seminars in Neurology. 45 (3): 410–419. doi:10.1055/a-2589-3825. PMID 40239951. TAK-360 is an oral SORA2þ that is chemically distinct from TAK-861 and developed to accommodate for higher and more flexible dosing that may be necessary for orexin normal populations, such as in NT2 or IH.100 TAK-360 is currently being evaluated in phase 2 dose-finding, adaptive, randomized, double-blinded, placebo-controlled trial to evaluate the safety, tolerability, and efficacy for individuals with IH.100
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