Details of the Drug

General Information of Drug (ID: DMBR01X)

Drug Name
Brilinta
Synonyms
Ticagrelor; 274693-27-5; Brilique; AZD-6140; AZD6140; AZD 6140; AR-C126532XX; UNII-GLH0314RVC; [14C]-Ticagrelor; GLH0314RVC; CHEBI:68558; (1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-DIFLUOROPHENYL)CYCLOPROPYL]AMINO]-5-(PROPYLTHIO)-3H-1,2,3-TRIAZOLO[4,5-D]PYRIMIDIN-3-YL]-5-(2-HYDROXYETHOXY)-1,2-CYCLOPENTANEDIOL; (1S,2S,3R,5S)-3-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol; Brilique; AR-C126532; Ticagrelor (USAN/INN); Brilinta/Brilique
Indication
Disease Entry ICD 11 Status REF
Thrombosis DB61-GB90 Approved [1], [2]
Arterial thrombosis DB61-DD30 Phase 3 [3]
Myocardial infarction BA41-BA43 Phase 3 [3]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 2 Molecular Weight (mw) 522.6
Topological Polar Surface Area (xlogp) 2
Rotatable Bond Count (rotbonds) 10
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 12
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 6675 mcgh/L [4]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 923 mcg/L [4]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.5 h [4]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [5]
Bioavailability
The bioavailability of drug is 36% [4]
Clearance
The renal clearance of drug is 0.00584 L/h [6]
Elimination
A radiolabelled dose of ticagrelor is 57.8% recovered in feces and 26.5% recovered in urine [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 8 hours [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.002% [7]
Vd
The volume of distribution (Vd) of drug is 88 L [4]
Chemical Identifiers
Formula
C23H28F2N6O4S
IUPAC Name
(1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
Canonical SMILES
CCCSC1=NC(=C2C(=N1)N(N=N2)[C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N[C@@H]4C[C@H]4C5=CC(=C(C=C5)F)F
InChI
InChI=1S/C23H28F2N6O4S/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28)/t12-,15+,16+,17-,19-,20+/m0/s1
InChIKey
OEKWJQXRCDYSHL-FNOIDJSQSA-N
Cross-matching ID
PubChem CID
9871419
ChEBI ID
CHEBI:68558
CAS Number
274693-27-5
DrugBank ID
DB08816
TTD ID
D0WF7L
VARIDT ID
DR00077
INTEDE ID
DR1591
ACDINA ID
D00674

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
P2Y purinoceptor 12 (P2RY12) TTZ1DT0 P2Y12_HUMAN Antagonist [8], [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [10]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [11]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Brilinta (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Metreleptin DM1NOEK Moderate Increased metabolism of Brilinta caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [35]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Brilinta caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [35]
Arn-509 DMT81LZ Major Increased metabolism of Brilinta caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [36]
Gilteritinib DMWQ4MZ Moderate Decreased metabolism of Brilinta caused by Gilteritinib mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [37]
Oliceridine DM6MDCF Moderate Decreased metabolism of Brilinta caused by Oliceridine mediated inhibition of CYP450 enzyme. Acute pain [MG31] [37]
Ivabradine DM0L594 Moderate Decreased metabolism of Brilinta caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [37]
Troleandomycin DMUZNIG Major Decreased metabolism of Brilinta caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [38]
Erdafitinib DMI782S Moderate Decreased clearance of Brilinta due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [39]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Brilinta caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [35]
LY2835219 DM93VBZ Moderate Decreased metabolism of Brilinta caused by LY2835219 mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [40]
Tucatinib DMBESUA Major Decreased metabolism of Brilinta caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [38]
Palbociclib DMD7L94 Moderate Decreased metabolism of Brilinta caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [37]
Macitentan DMP79A1 Moderate Decreased metabolism of Brilinta caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [41]
PF-04449913 DMSB068 Moderate Decreased metabolism of Brilinta caused by PF-04449913 mediated inhibition of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [42]
Levomilnacipran DMV26S8 Moderate Increased risk of bleeding by the combination of Brilinta and Levomilnacipran. Chronic pain [MG30] [43]
Fidaxomicin DMFP6MV Minor Decreased clearance of Brilinta due to the transporter inhibition by Fidaxomicin. Clostridium difficile enterocolitis [1A04] [38]
Regorafenib DMHSY1I Major Increased risk of bleeding by the combination of Brilinta and Regorafenib. Colorectal cancer [2B91] [37]
Intedanib DMSTA36 Moderate Increased risk of bleeding by the combination of Brilinta and Intedanib. Colorectal cancer [2B91] [44]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Brilinta caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [37]
Lumacaftor DMCLWDJ Major Increased metabolism of Brilinta caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [45]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Brilinta caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [37]
MK-8228 DMOB58Q Moderate Decreased metabolism of Brilinta caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [37]
Vortioxetine DM6F1PU Moderate Increased risk of bleeding by the combination of Brilinta and Vortioxetine. Depression [6A70-6A7Z] [43]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Brilinta caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [46]
Apigenin DMI3491 Minor Increased risk of bleeding by the combination of Brilinta and Apigenin. Discovery agent [N.A.] [47]
Stiripentol DMMSDOY Moderate Decreased metabolism of Brilinta caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [37]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Brilinta caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [35]
Bay 80-6946 DMLOS5R Moderate Decreased clearance of Brilinta due to the transporter inhibition by Bay 80-6946. Follicular lymphoma [2A80] [48]
Tazemetostat DMWP1BH Moderate Decreased metabolism of Brilinta caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [49]
Mirabegron DMS1GYT Minor Decreased metabolism of Brilinta caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [50]
Avapritinib DMK2GZX Major Increased risk of bleeding by the combination of Brilinta and Avapritinib. Gastrointestinal stromal tumour [2B5B] [37]
Boceprevir DMBSHMF Major Decreased metabolism of Brilinta caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [38]
GS-5885 DMSL3DX Moderate Decreased clearance of Brilinta due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [51]
MK-1439 DM215WE Minor Decreased metabolism of Brilinta caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [52]
Cobicistat DM6L4H2 Major Decreased metabolism of Brilinta caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [38]
Dolutegravir DMCZGRE Minor Decreased metabolism of Brilinta caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [53]
BMS-201038 DMQTAGO Moderate Decreased clearance of Brilinta due to the transporter inhibition by BMS-201038. Hyper-lipoproteinaemia [5C80] [54]
Aliskiren DM1BV7W Moderate Decreased clearance of Brilinta due to the transporter inhibition by Aliskiren. Hypertension [BA00-BA04] [35]
Lesinurad DMUR64T Moderate Increased metabolism of Brilinta caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [35]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Brilinta caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [37]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Brilinta caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [38]
Naloxegol DML0B41 Minor Decreased clearance of Brilinta due to the transporter inhibition by Naloxegol. Large intestine motility disorder [DB32] [55]
Crizotinib DM4F29C Moderate Decreased metabolism of Brilinta caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [37]
Brigatinib DM7W94S Moderate Increased metabolism of Brilinta caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [35]
Ceritinib DMB920Z Major Decreased metabolism of Brilinta caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [38]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Brilinta caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [56]
PF-06463922 DMKM7EW Moderate Increased metabolism of Brilinta caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [35]
Osimertinib DMRJLAT Moderate Decreased metabolism of Brilinta caused by Osimertinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [57]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Brilinta caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [58]
Capmatinib DMYCXKL Moderate Decreased clearance of Brilinta due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [59]
Selpercatinib DMZR15V Moderate Decreased metabolism of Brilinta caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [37]
Calaspargase pegol DMQZBXI Moderate Increased risk of bleeding by the combination of Brilinta and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [60]
Idelalisib DM602WT Major Decreased metabolism of Brilinta caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [38]
GDC-0199 DMH0QKA Major Decreased clearance of Brilinta due to the transporter inhibition by GDC-0199. Mature B-cell leukaemia [2A82] [38]
IPI-145 DMWA24P Moderate Decreased metabolism of Brilinta caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [37]
Acalabrutinib DM7GCVW Major Increased risk of bleeding by the combination of Brilinta and Acalabrutinib. Mature B-cell lymphoma [2A85] [61]
Ibrutinib DMHZCPO Major Increased risk of bleeding by the combination of Brilinta and Ibrutinib. Mature B-cell lymphoma [2A85] [62]
Ponatinib DMYGJQO Major Increased risk of bleeding by the combination of Brilinta and Ponatinib. Mature B-cell lymphoma [2A85] [63]
Arry-162 DM1P6FR Moderate Decreased clearance of Brilinta due to the transporter inhibition by Arry-162. Melanoma [2C30] [38]
Vemurafenib DM62UG5 Moderate Increased metabolism of Brilinta caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [35]
LGX818 DMNQXV8 Moderate Increased metabolism of Brilinta caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [64]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Brilinta caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [37]
Ubrogepant DM749I3 Moderate Decreased clearance of Brilinta due to the transporter inhibition by Ubrogepant. Migraine [8A80] [65]
Lasmiditan DMXLVDT Moderate Decreased clearance of Brilinta due to the transporter inhibition by Lasmiditan. Migraine [8A80] [66]
Fedratinib DM4ZBK6 Moderate Increased risk of bleeding by the combination of Brilinta and Fedratinib. Myeloproliferative neoplasm [2A20] [37]
Ruxolitinib DM7Q98D Moderate Increased risk of bleeding by the combination of Brilinta and Ruxolitinib. Myeloproliferative neoplasm [2A20] [37]
Vorapaxar DMA16BR Moderate Increased risk of bleeding by the combination of Brilinta and Vorapaxar. Myocardial infarction [BA41-BA43] [37]
Rolapitant DM8XP26 Moderate Decreased clearance of Brilinta due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [67]
Netupitant DMEKAYI Moderate Decreased metabolism of Brilinta caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [37]
Entrectinib DMMPTLH Moderate Decreased metabolism of Brilinta caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [68]
S-297995 DM26IH8 Moderate Decreased clearance of Brilinta due to the transporter inhibition by S-297995. Opioid use disorder [6C43] [37]
Olaparib DM8QB1D Moderate Decreased metabolism of Brilinta caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [69]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Brilinta caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [70]
MK-4827 DMLYGH4 Moderate Increased risk of bleeding by the combination of Brilinta and MK-4827. Ovarian cancer [2C73] [37]
Abametapir DM2RX0I Moderate Decreased metabolism of Brilinta caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [71]
Lefamulin DME6G97 Moderate Decreased metabolism of Brilinta caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [72]
Choline salicylate DM8P137 Moderate Increased risk of bleeding by the combination of Brilinta and Choline salicylate. Postoperative inflammation [1A00-CA43] [37]
Enzalutamide DMGL19D Major Increased metabolism of Brilinta caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [36]
Relugolix DMK7IWL Major Decreased clearance of Brilinta due to the transporter inhibition by Relugolix. Prostate cancer [2C82] [73]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Brilinta caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [37]
LDE225 DMM9F25 Moderate Decreased metabolism of Brilinta caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [74]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Brilinta caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [37]
Larotrectinib DM26CQR Moderate Decreased metabolism of Brilinta caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [38]
LEE011 DMMX75K Moderate Decreased metabolism of Brilinta caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [37]
Curcumin DMQPH29 Minor Increased risk of bleeding by the combination of Brilinta and Curcumin. Solid tumour/cancer [2A00-2F9Z] [75]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Brilinta caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [76]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Brilinta due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [70]
Cabozantinib DMIYDT4 Major Increased risk of bleeding by the combination of Brilinta and Cabozantinib. Thyroid cancer [2D10] [77]
Elagolix DMB2C0E Moderate Increased metabolism of Brilinta caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [35]
Betrixaban DM2C4RF Major Increased risk of bleeding by the combination of Brilinta and Betrixaban. Venous thromboembolism [BD72] [78]
⏷ Show the Full List of 90 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Brushite E00392 104805 Diluent
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Water E00035 962 Solvent
⏷ Show the Full List of 10 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Ticagrelor 60 mg tablet 60 mg Oral Tablet Oral
Ticagrelor 90 mg tablet 90 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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58 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
59 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
60 Caruso V, Iacoviello L, Di Castelnuovo A, et.al "Thrombotic complications in childhood acute lymphoblastic leukemia: a meta-analysis of 17 prospective studies comprising 1752 pediatric patients." Blood 108 (2006): 2216-22. [PMID: 16804111]
61 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
62 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
63 Product Information. Iclusig (ponatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
64 Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
65 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
66 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
67 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
68 Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
69 Product Information. Lynparza (olaparib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
70 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
71 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
72 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
73 Product Information. Orgovyx (relugolix). Myovant Sciences, Inc., Brisbane, CA.
74 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
75 Abebe W "Herbal medication: potential for adverse interactions with analgesic drugs." J Clin Pharm Ther 27 (2002): 391-401. [PMID: 12472978]
76 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
77 Product Information. Cometriq (cabozantinib). Exelixis Inc, S San Francisco, CA.
78 Product Information. Bevyxxa (betrixaban). Portola Pharmaceuticals, South San Francisco, CA.