241:
29:
509:
Basimglurant has shown the desired characteristics of a drug with high bioavailability, few safety liabilities, and promise in the secondary endpoints of a phase IIb trial. Basimglurant will most likely undergo future iterations and attempt to pass drug trials again due to the large investment
428:
It was discovered in a medicinal chemistry effort conducted at Roche starting from the results of a small molecular weight compound library high-throughput screen based on a Ca21 mobilization assay with human mGlu5a (Jaeschke et al., 2015). The high-throughput screen identified several mGlu5
518:
Basimglurant was originally developed for the treatment of fragile X syndrome, but after failing phase II clinical trials Roche abandoned the drug in this field of application and is renewing basimglurant as part of a treatment for depression.
781:
501:
Phase II clinical trials have been undertaken, and a lack of efficacy was found overall. Improved secondary endpoints though of 1.5 mg dosage has prompted future clinical trials of the drug.
1843:
774:
498:
cohort. The trial was undertaken to study (and verify) the safety of basimglurant as a potential drug. Completion of this trial allowed for basimglurant to begin phase II drug trials.
1793:
686:
for "A Study of the Safety, Tolerability, and
Pharmacokinetics of Multiple-Ascending Dose Basimglurant in Healthy Subjects and in Patients With Major Depressive Disorder (MDD)" at
53:
767:
1789:
474:
of 7 hours in rats and 20 hours in monkeys, indicating a dosing regimen of once daily in possible human patients. Research with rats and monkeys revealed a
642:"Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression"
328:
1347:
1206:
963:
490:
Phase I clinical trials for basimglurant began in April 2015, and finished in
September 2015. 56 people were spread out among 4 healthy cohorts, a
1813:
528:
441:. In partnership with Chugai Pharmaceutical, basimglurant is currently still undergoing revision from previous drug trials as of November 2016.
740:
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180:
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574:
550:
958:
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403:
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1818:
701:"Efficacy and Safety of Basimglurant as Adjunctive Therapy for Major Depression: A Randomized Clinical Trial"
1332:
1184:
41:
356:
InChI=1S/C18H13ClFN3/c1-12-17(8-3-14-9-10-21-18(19)11-14)22-13(2)23(12)16-6-4-15(20)5-7-16/h4-7,9-11H,1-2H3
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Lindemann L, Porter RH, Scharf SH, Kuennecke B, Bruns A, von
Kienlin M, et al. (April 2015).
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914:
741:"Roche abandons another Fragile X R&D program after PhII trials flunk out | FierceBiotech"
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Quiroz JA, Tamburri P, Deptula D, Banken L, Beyer U, Rabbia M, et al. (July 2016).
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1307:
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894:
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Preclinical research trials found that basimglurant has a high specificity for the
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20:
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28:
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of 50%, with additional studies showing that basimglurant has a rate of
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Preclinical drug trials showed that basimglurant possessed a
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The
Journal of Pharmacology and Experimental Therapeutics
510:
already poured into the drug to develop it this far.
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1844:Glutamate receptor negative allosteric modulators
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1794:Glutamate metabolism/transport modulators
1701:Tooltip Metabotropic glutamate receptor 8
1602:Tooltip Metabotropic glutamate receptor 7
1530:Tooltip Metabotropic glutamate receptor 6
1426:Tooltip Metabotropic glutamate receptor 4
1277:Tooltip Metabotropic glutamate receptor 3
1119:Tooltip Metabotropic glutamate receptor 2
933:Tooltip Metabotropic glutamate receptor 5
819:Tooltip Metabotropic glutamate receptor 1
716:
657:
188:
1790:Ionotropic glutamate receptor modulators
418:. As of November 2016, it has undergone
539:
529:List of investigational antidepressants
353:
336:Clc3nccc(C#Cc2nc(n(c1ccc(F)cc1)c2C)C)c3
333:
235:
103:
18:
7:
1333:Pomaglumetad methionil (LY-2140023)
1185:Pomaglumetad methionil (LY-2140023)
208:
139:
575:"Roche Group Development Pipeline"
14:
718:10.1001/jamapsychiatry.2016.0838
615:. Springer Nature Switzerland AG
280:
277:
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1729:Positive allosteric modulators:
1680:Negative allosteric modulators:
1469:Positive allosteric modulators:
1387:Negative allosteric modulators:
1251:Negative allosteric modulators:
1194:Positive allosteric modulators:
1050:Negative allosteric modulators:
993:Positive allosteric modulators:
791:Metabotropic glutamate receptor
425:for both of these indications.
361:Key:UPZWINBEAHDTLA-UHFFFAOYSA-N
1814:Drugs not assigned an ATC code
408:treatment-resistant depression
398:which is under development by
262:
1:
1786:Receptor/signaling modulators
388:negative allosteric modulator
378:) (developmental code names
106:2-chloro-4-{ethynyl}pyridine
1865:
1824:MGlu5 receptor antagonists
252:Chemical and physical data
1779:
1318:LY-404,039 (pomaglumetad)
1165:LY-404,039 (pomaglumetad)
492:major depressive disorder
344:
324:
94:
26:
1849:4-Fluorophenyl compounds
1197:JNJ-40411813 (ADX-71149)
659:10.1124/jpet.114.222463
680:Clinical trial number
580:. 2014. Archived from
480:plasma protein binding
745:www.fiercebiotech.com
406:for the treatment of
404:Chugai Pharmaceutical
429:antagonists such as
1834:4-Pyridyl compounds
450:Mechanism of action
23:
1839:Alkyne derivatives
688:ClinicalTrials.gov
551:"Roche - Pipeline"
472:terminal half-life
456:glutamate receptor
416:fragile X syndrome
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315:Interactive image
221:CompTox Dashboard
16:Chemical compound
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1829:Chloropyridines
1819:Antidepressants
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984:Quisqualic acid
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609:"Basimglurant"
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494:cohort, and a
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1316:
1314:
1311:
1309:
1308:Ibotenic acid
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1155:Ibotenic acid
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979:Ibotenic acid
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895:Cyclothiazide
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845:Ibotenic acid
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711:(7): 675–84.
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669:
665:
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652:(1): 213–33.
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598:
587:on 2014-08-08
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36:Clinical data
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30:
25:
1782:
1781:
1739:Antagonists:
1738:
1728:
1708:
1679:
1638:Antagonists:
1637:
1609:
1556:Antagonists:
1555:
1537:
1484:Antagonists:
1483:
1468:
1433:
1386:
1345:Antagonists:
1344:
1338:Talaglumetad
1284:
1250:
1204:Antagonists:
1203:
1193:
1190:Talaglumetad
1126:
1063:Dipraglurant
1058:Basimglurant
1057:
1049:
1003:Antagonists:
1002:
992:
940:
882:Antagonists:
881:
826:
748:. Retrieved
744:
735:
708:
704:
694:
681:
676:
649:
645:
617:. Retrieved
613:Adis Insight
612:
589:. Retrieved
582:the original
555:. Retrieved
517:
508:
500:
489:
469:
453:
445:Pharmacology
427:
383:
379:
372:Basimglurant
371:
370:
75:Legal status
69:Legal status
21:Basimglurant
1465:VU-0155,041
1390:Decoglurant
1254:Decoglurant
1088:Raseglurant
1036:Remeglurant
1021:Mavoglurant
885:BAY 36-7620
683:NCT02433093
298: g·mol
125:802906-73-6
90:Identifiers
1808:Categories
1732:AZ12216052
1472:Foliglurax
1460:VU-001,171
1373:LY-341,495
1368:LY-307,452
1323:LY-487,379
1313:LY-379,268
1232:LY-341,495
1227:LY-307,452
1175:LY-566,332
1170:LY-487,379
1160:LY-379,268
1016:LY-344,545
996:LSN2463359
905:LY-456,236
900:LY-367,385
794:modulators
750:2016-11-20
619:2016-11-20
591:2014-08-01
557:2014-08-01
535:References
384:RO-4917523
303:3D model (
291:Molar mass
190:3110E3AO8S
161:ChemSpider
116:CAS Number
99:IUPAC name
1783:See also:
1717:Glutamate
1709:Agonists:
1631:LSP2-9166
1618:Glutamate
1610:Agonists:
1541:Glutamate
1538:Agonists:
1450:LSP2-9166
1437:Glutamate
1434:Agonists:
1409:Group III
1395:RO4491533
1303:Glutamate
1298:Eglumegad
1285:Agonists:
1259:RO4491533
1150:Glutamate
1145:Eglumegad
1127:Agonists:
974:Glutamate
949:ADX-47273
941:Agonists:
865:Ro67-7476
860:Ro67-4853
855:Ro01-6128
840:Glutamate
827:Agonists:
42:Routes of
1767:UBP-1112
1683:ADX71743
1671:UBP-1112
1584:UBP-1112
1512:UBP-1112
1383:MGS-0039
1328:MGS-0028
1242:MGS-0039
1180:MGS-0028
1102:Group II
1046:SIB-1893
1041:SIB-1757
1031:NPS-2390
915:NPS-2390
875:Theanine
727:27304433
668:25665805
523:See also
420:phase II
396:receptor
150:11438771
54:ATC code
48:By mouth
1073:GRN-529
1068:Fenobam
1053:AZD9272
989:VU-1545
890:CPCCOEt
802:Group I
514:History
496:placebo
439:fenobam
412:adjunct
410:(as an
390:of the
386:) is a
380:RG-7090
258:Formula
170:9613635
136:PubChem
1676:XAP044
1613:AMN082
1293:DCG-IV
1288:CBiPES
1247:PCCG-4
1140:DCG-IV
1135:CBiPES
725:
666:
553:. 2014
505:Future
437:, and
414:) and
329:SMILES
296:325.77
210:D10864
1694:mGluR
1651:MMPIP
1595:mGluR
1523:mGluR
1455:PHCCC
1419:mGluR
1363:HYDIA
1353:CECXG
1348:APICA
1270:mGluR
1222:HYDIA
1212:CECXG
1207:APICA
1112:mGluR
1011:DMeOB
954:CDPPB
926:mGluR
870:VU-71
812:mGluR
585:(PDF)
578:(PDF)
400:Roche
349:InChI
305:JSmol
1762:MTPG
1757:MSOP
1752:MPPG
1747:MAP4
1742:CPPG
1725:-AP4
1712:DCPG
1666:MTPG
1661:MSOP
1656:MPPG
1646:MAP4
1641:CPPG
1626:-AP4
1579:MTPG
1574:MSOP
1569:MPPG
1564:MAP4
1559:CPPG
1549:-AP4
1507:MTPG
1502:MSOP
1497:MPPG
1492:MAP4
1487:CPPG
1477:MPEP
1445:-AP4
1378:MCPG
1358:EGLU
1237:MCPG
1217:EGLU
1130:BINA
1083:MTEP
1078:MPEP
1026:MCPG
1006:CTEP
969:DHPG
959:CHPG
944:ACPD
910:MCPG
835:DHPG
830:ACPD
723:PMID
664:PMID
458:mGlu
435:MTEP
431:MPEP
402:and
392:mGlu
201:KEGG
181:UNII
61:none
964:DFB
713:doi
654:doi
650:353
376:INN
226:EPA
140:CID
1810::
1792:•
1788:•
1727:;
1678:;
1467:;
1385:;
1249:;
1192:;
1048:;
991:;
743:.
721:.
709:73
707:.
703:.
662:.
648:.
644:.
628:^
611:.
600:^
566:^
542:^
433:,
382:,
275:Cl
272:13
266:18
1723:L
1696:8
1624:L
1597:7
1547:L
1525:6
1443:L
1421:4
1272:3
1114:2
928:5
814:1
783:e
776:t
769:v
753:.
729:.
715::
670:.
656::
622:.
594:.
560:.
460:5
394:5
374:(
307:)
284:3
281:N
278:F
269:H
263:C
228:)
224:(
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