Drug Information

Drug (ID: DG00952) and It's Reported Resistant Information

• Name: Brinzolamide
• Synonyms: Brinzolamide; 138890-62-7; Azopt; AL-4862; AL 4862; Birnzolamide; (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide; MFCD08067749; UNII-9451Z89515; (4R)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide; 138890-50-3; CHEBI:3176; (R)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide; (+)-4-ETHYLAMINO-3,4-DIHYDRO-2-(METHOXY)PROPYL-2H-THIENO[3,2-E]-1,2-THIAZINE-6-SULFONAMIDE-1,1-DIOXIDE; (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno(3,2-e)-1,2-thiazine-6-sulfonamide 1,1-dioxide; (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide; DSSTox_CID_25531; DSSTox_RID_80934; DSSTox_GSID_45531; 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-; BZ1; 9451Z89515; C12H21N3O5S3; (4R)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide; Brinzolamide (BRZ); Azopt (TN); Brinzolamide (JAN/USP/INN); 3znc; NSC-760050; NCGC00016979-01; Brinzolamide [USAN:USP:INN:BAN]; Brinzolamide- Bio-X; CAS-138890-62-7; Prestwick0_000365; Prestwick1_000365; Prestwick2_000365; Prestwick3_000365; SCHEMBL24636; BSPBio_000489; 2H-Thieno(3,2-e)-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (R)-; MLS002153787; BIDD:GT0039; SPBio_002410; AMY372; BPBio1_000539; CHEMBL220491; GTPL6797; DTXSID6045531; BDBM10885; Brinzolamide, >=98% (HPLC); HMS1569I11; HMS2096I11; HMS2234K06; HMS3713I11; HMS3885I11; BCP22330; HY-B0588; ZINC3953037; Tox21_110722; s3178; AKOS005145708; Tox21_110722_1; AC-5277; CCG-220365; CCG-222516; DB01194; NSC 760050; NCGC00179542-03; NCGC00179542-09; NCGC00179542-10; AS-35084; BB164262; SMR001233169; AB00513824; B4258; SW197152-3; AL4862;AL 4862;AL-4862; C07760; D00652; AB00513824_06; Q411517; SR-01000838832; Q-200751; SR-01000838832-2; BRD-K74913225-001-03-3; Brinzolamide, United States Pharmacopeia (USP) Reference Standard; (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1$l^{6},7,2-thieno[3,2-e][1$l^{6},2]thiazine-6-sulfonamide; (4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1$l^{6},7,2-thieno[3,2-e][1,2]thiazine-6-sulfonamide; (4r)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2h-thieno[3,2-e][1,2]thiazine-6-sulfonamide-1,1-dioxide; (4R)-4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[4,5-e]thiazine-6-sulfonamide; (5R)-5-ethylamino-3-(3-methoxypropyl)-2,2-dioxo-2,9-dithia-3-azabicyclo[4.3.0]nona-1(6)7-diene-8-sulfonamide; (5R)-5-Ethylamino-3-(3-methoxypropyl)-2,2-dioxo-2 6,9-dithia-3-azabicyclo[4.3.0]nona-7,10-diene-8-sulfonamide; (R)- 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide; (R)-3,4-Dihydro-4-ethylamino-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide; 2H-Thieno(3,2-e)-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-,1,1-dioxide, (R)-
• Indication:
  In total 1 Indication(s)
  Open-angle glaucoma [ICD-11: 9C61]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Asthma [ICD-11: CA23]; [1]
• Target: Carbonic anhydrase IV (CA-IV); CAH4_HUMAN; [1]
• Formula: C12H21N3O5S3
• IsoSMILES: CCN[C@H]1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
• InChI: 1S/C12H21N3O5S3/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17)/t10-/m0/s1
• InChIKey: HCRKCZRJWPKOAR-JTQLQIEISA-N
• PubChem CID: 68844
• ChEBI ID: CHEBI:3176
• TTD Drug ID: D01MUR
• INTEDE ID: DR0229
• DrugBank ID: DB01194

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-12: Respiratory system diseases

Asthma [ICD-11: CA23]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Interleukin-1 beta (IL1B) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Asthma [ICD-11: CA23.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549/NF-kappaB-luc reporter cells; Lung; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: NF-kappaB activity assay
• Mechanism Description: Corticosteroid resistance causes significant morbidity in asthma, and drug repurposing may identify timely and cost-effective adjunctive treatments for corticosteroid resistance. gamma-linolenic acid, brinzolamide, and INCA-6 significantly reduced IL-1beta induced luciferase activity and potentiated the anti-inflammatory effect of dexamethasone in A549/NF-kappaB-luc reporter cells. These results demonstrate how existing drugs, including gamma-linolenic acid, brinzolamide, and INCA-6, may be repurposed to improve corticosteroid response in asthmatics.

References

• Ref 1: Drug Repurposing to Treat Glucocorticoid Resistance in Asthma .J Pers Med. 2021 Mar 3;11(3):175. doi: 10.3390/jpm11030175. 10.3390/jpm11030175