Balumorexton

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]

Other namesTAK-360; TAK360

Routes of
administrationOral^[1]

Drug classOrexin OX₂ receptor antagonist; Wakefulness-promoting agent

CAS Number

3037907-48-2

Quick facts Clinical data, Other names ...

Balumorexton
Clinical data

Other names	TAK-360; TAK360
Routes of administration	Oral^[1]
Drug class	Orexin OX₂ receptor antagonist; Wakefulness-promoting agent
Identifiers
IUPAC name 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	3037907-48-2
PubChem CID	171548344
UNII	NE3ZS9HSP2
Chemical and physical data
Formula	C₂₀H₁₂F₆N₄O₄S
Molar mass	518.39 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES 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 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

References

[1]
"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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