TAK-994

TAK-994Clinical data

Routes of
administration| Oral[1]
Drug class| Orexin receptor agonist

TAK-994 is an orexin receptor agonist which is under development by Takeda for the treatment of narcolepsy.[2][3] It is a small-molecule and orally active compound and acts as a highly selective agonist of the orexin receptor 2 (OX2) (>700-fold selectivity over the orexin receptor 1 (OX1)).[2][3][4][1] TAK-994 is related to danavorexton (TAK-925).[5] The compound reached phase 2 clinical trials for narcolepsy.[6] However, clinical development was discontinued in October 2021 for safety reasons.[5][7][8][9][10] The chemical structure of TAK-994 has yet to be disclosed.[4]

## See also[edit]

* Orexin receptor § Agonists
* List of investigational sleep drugs § Orexin receptor agonists

## References[edit]

1. ^ a b Pellitteri G, de Biase S, Valente M, Gigli GL (August 2021). "How treatable is narcolepsy with current pharmacotherapy and what does the future hold?". Expert Opinion on Pharmacotherapy. 22 (12): 1517–1520. doi:10.1080/14656566.2021.1915987. PMID 33882765. S2CID 233349300.
2. ^ a b Ishikawa T, Suzuki M, Kimura H (April 2020). "0141 A Novel, Orally Available Orexin 2 Receptor-Selective Agonist, TAK-994, Shows Wake-Promoting Effects Following Chronic Dosing in an Orexin-Deficient Narcolepsy Mouse Model". Sleep. 43 (Supplement 1): A56. doi:10.1093/sleep/zsaa056.139. eISSN 1550-9109. ISSN 0161-8105.
3. ^ a b Thorpy MJ (January 2020). "Recently Approved and Upcoming Treatments for Narcolepsy". CNS Drugs. 34 (1): 9–27. doi:10.1007/s40263-019-00689-1. PMC 6982634. PMID 31953791.
4. ^ a b Zhang D, Perrey DA, Decker AM, Langston TL, Mavanji V, Harris DL, et al. (June 2021). "Discovery of Arylsulfonamides as Dual Orexin Receptor Agonists". Journal of Medicinal Chemistry. 64 (12): 8806–8825. doi:10.1021/acs.jmedchem.1c00841. PMC 8994207. PMID 34101446.
5. ^ a b Jacobson LH, Hoyer D, de Lecea L (January 2022). "Hypocretins (orexins): The ultimate translational neuropeptides". J Intern Med. 291 (5): 533–556. doi:10.1111/joim.13406. PMID 35043499. S2CID 248119793.
6. ^ Clinical trial number NCT04096560 for "A Study of TAK-994 in Adults With Type 1 and Type 2 Narcolepsy" at ClinicalTrials.gov
7. ^ "Takeda Provides Update on TAK-994 Clinical Program". Business Wire. 5 October 2021.
8. ^ "Takeda pauses TAK-994 clinical studies due to safety glitch". The Pharma Letter. 6 October 2021.
9. ^ Jackson M (6 October 2021). "Takeda Halts Phase II Studies For Key R&D Asset TAK-994 In Narcolepsy". Scrip. Informa Pharma Intelligence.
10. ^ Tong A (6 October 2021). "Takeda flashes red light on 'breakthrough' narcolepsy drug after PhII trials turned up mysterious safety signal". Endpoints News.

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* t
* e

Orexin receptor modulators

OX1|

* Agonists: Orexin (A, B)

* Antagonists: ACT-335827
* ACT-462206
* ACT-539313
* Almorexant
* AZD-4041
* C4X-3256 (INDV-2000)
* CR-5542
* Daridorexant
* Filorexant
* GSK-649868 (SB-649868)
* JNJ-61393215
* Lemborexant
* RTIOX-276
* SB-334867
* SB-408124
* Suvorexant
* TCS-1102
* Vornorexant (ORN-0829, TS-142)
* YZJ-1139

OX2|

* Agonists: Danavorexton (TAK-925)
* Firazorexton
* Orexin (A, B)
* SB-668875
* Suntinorexton
* TAK-861
* TAK-994

* Antagonists: ACT-335827
* ACT-462206
* Almorexant
* Daridorexant
* EMPA
* Filorexant
* GSK-649868 (SB-649868)
* JNJ-10397049
* Lemborexant
* MK-1064
* MK-3697
* MK-8133
* Seltorexant
* Suvorexant
* TCS-1102
* TCS-OX2-29
* Vornorexant (ORN-0829, TS-142)
* YZJ-1139

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