Balovaptan

Balovaptan
Clinical data
Other names	RG7314
Legal status
Legal status	US: ℞-only ;
Identifiers
	IUPAC name 8-Chloro-5-methyl-1-(4-pyridin-2-yloxycyclohexyl)-4,6-dihydro-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine;
CAS Number	1228088-30-9;
PubChem CID	46200932;
DrugBank	DB14823;
ChemSpider	59718648;
UNII	RAX5D5AGV6;
KEGG	D11476;
Chemical and physical data
Formula	C22H24ClN5O
Molar mass	409.92 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1CC2=NN=C([C@H]3CC[C@@H](CC3)OC3=CC=CC=N3)N2C2=C(C1)C=C(Cl)C=C2;
	InChI InChI=1S/C22H24ClN5O/c1-27-13-16-12-17(23)7-10-19(16)28-20(14-27)25-26-22(28)15-5-8-18(9-6-15)29-21-4-2-3-11-24-21/h2-4,7,10-12,15,18H,5-6,8-9,13-14H2,1H3/t15-,18-; Key:GMPZPHGHNDMRKL-RZDIXWSQSA-N;

Balovaptan (INN; developmental code name RG7314), is a selective small molecule antagonist of the vasopressin V_1A receptor which is under development by Roche for the treatment of autism.^[1] As of August 2019, it is in a phase III clinical trial for adults and a phase II clinical trial for children for this indication.^[2] On 29 January 2018, Roche announced that the US Food and Drug Administration (FDA) had granted Breakthrough Therapy Designation for balovaptan in individuals with autism spectrum disorder (ASD).^[3] The FDA granted this based on the results of the adult phase II clinical trial called VANILLA (Vasopressin ANtagonist to Improve sociaL communication in Autism) study.^[4] The currently-recruiting (Until March 2020) phase III adult study is called V1aduct and the currently-closed (August 2019) phase II child study is called Av1ation.^{[citation needed]}

References[edit]

^ "Roche - Pipeline". 2014. Retrieved 1 August 2014.
^ Clinical trial number NCT01793441 for "Study of RG7314 to Investigate Efficacy and Safety in Individuals With Autism Spectrum Disorders" at ClinicalTrials.gov
^ "FDA grants Breakthrough Therapy Designation for Roche's balovaptan in autism spectrum disorder" (Press release). 29 January 2018. Retrieved 6 February 2018.
^ Bolognani F, Del Valle Rubido M, Squassante L, Wandel C, Derks M, Murtagh L, et al. (May 2019). "A phase 2 clinical trial of a vasopressin V1a receptor antagonist shows improved adaptive behaviors in men with autism spectrum disorder". Science Translational Medicine. 11 (491). doi:10.1126/scitranslmed.aat7838. PMID 31043521.

External links[edit]

"Balovaptan". Drug Information Portal. U.S. National Library of Medicine.

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[Roche2014-1] "Roche - Pipeline". 2014. Retrieved 1 August 2014.

[ClinicalTrialsDotGov-2] Clinical trial number NCT01793441 for "Study of RG7314 to Investigate Efficacy and Safety in Individuals With Autism Spectrum Disorders" at ClinicalTrials.gov

[290118PressRelease-3] "FDA grants Breakthrough Therapy Designation for Roche's balovaptan in autism spectrum disorder" (Press release). 29 January 2018. Retrieved 6 February 2018.

[4] Bolognani F, Del Valle Rubido M, Squassante L, Wandel C, Derks M, Murtagh L, et al. (May 2019). "A phase 2 clinical trial of a vasopressin V1a receptor antagonist shows improved adaptive behaviors in men with autism spectrum disorder". Science Translational Medicine. 11 (491). doi:10.1126/scitranslmed.aat7838. PMID 31043521.

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v t e Benzodiazepines
1,4-Benzodiazepines	2-Oxoquazepam 3-Hydroxyphenazepam Bromazepam BMS-906024* Camazepam Carburazepam Chlordiazepoxide Cinazepam Cinolazepam Clonazepam Cloniprazepam Clorazepate Cyprazepam Delorazepam Demoxepam Desmethylflunitrazepam Devazepide* Diazepam Diclazepam Difludiazepam Doxefazepam Elfazepam Ethyl carfluzepate Ethyl dirazepate Ethyl loflazepate Flubromazepam Fletazepam Fludiazepam Flunitrazepam Flurazepam Flutemazepam Flutoprazepam Fosazepam Gidazepam Halazepam Iclazepam Irazepine Kenazepine Ketazolam Lorazepam Lormetazepam Lufuradom* Meclonazepam Medazepam Menitrazepam Metaclazepam Motrazepam N-Desalkylflurazepam Nifoxipam Nimetazepam Nitemazepam Nitrazepam Nitrazepate Nordazepam Nortetrazepam Oxazepam Phenazepam Pinazepam Pivoxazepam Prazepam Proflazepam Quazepam QH-II-66 Reclazepam RO4491533* Ro05-4082 Ro5-4864* SH-I-048A Sulazepam Temazepam Tetrazepam Tifluadom* Timelotem* Tolufazepam Triflunordazepam Tuclazepam Uldazepam
1,5-Benzodiazepines	Arfendazam Clobazam CP-1414S Lofendazam Triflubazam
2,3-Benzodiazepines*	Girisopam GYKI-52466 GYKI-52895 Nerisopam Talampanel Tofisopam
Triazolobenzodiazepines	Adinazolam Alprazolam Balovaptan* Bromazolam Phenazolam Rilmazolam (active metabolite of Rilmazafone) Clonazolam Estazolam Flualprazolam Flubromazolam Flunitrazolam Nitrazolam Pyrazolam Triazolam
Imidazobenzodiazepines	Bretazenil Climazolam EVT-201 FG-8205 Flumazenil GL-II-73 Imidazenil ¹²³I-Iomazenil L-655,708 Loprazolam Midazolam PWZ-029 Remimazolam Ro15-4513 Ro48-6791 Ro48-8684 Ro4938581 Sarmazenil SH-053-R-CH3-2′F
Oxazolobenzodiazepines	Cloxazolam Flutazolam Haloxazolam Mexazolam Oxazolam
Thienodiazepines	Bentazepam Clotiazepam
Thienotriazolodiazepines	Brotizolam Ciclotizolam Deschloroetizolam Etizolam Fluclotizolam Israpafant* JQ1* Metizolam
Thienobenzodiazepines*	Olanzapine Telenzepine
Pyridodiazepines	Lopirazepam
Pyridotriazolodiazepines	Zapizolam
Pyrazolodiazepines	Razobazam* Ripazepam Zolazepam Zomebazam Zometapine*
Pyrrolodiazepines	Premazepam
Tetrahydroisoquinobenzodiazepines	Clazolam
Pyrrolobenzodiazepines*	Anthramycin
Benzodiazepine prodrugs	Alprazolam triazolobenzophenone Avizafone Rilmazafone
* atypical activity profile (not GABA_A receptor ligands)

Balovaptan

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References[edit]

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