ticarcillin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, 6-aminopenicillanic acid derivatives 2656 34787-01-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ticarcillin
  • ticarcillin disodium
  • ticarcillin sodium
An antibiotic derived from penicillin similar to CARBENICILLIN in action.
  • Molecular weight: 384.42
  • Formula: C15H16N2O6S2
  • CLOGP: 1.28
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 124.01
  • ALOGS: -3.73
  • ROTB: 5
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
15 g P
15 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1000 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 77 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 780.37 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.16 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.55 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -2.369 High 0.82
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.494 High 0.82
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.336 10^-6 cm/s High 0.82
dh-clint Dog hepatocyte intrinsic clearance 3.141 uL/min/10^6 cells High 0.82
dppb Dog plasma protein binding (% unbound) 61.910 % High 0.82
fcs-ppb Fetal calf serum protein binding (% unbound) 44.550 % High 0.82
herg hERG pIC50 4.507 pIC50 High 0.82
hh-clint Human hepatocyte intrinsic clearance 1.327 uL/min/10^6 cells High 0.82
hlm-clint Human liver microsomal intrinsic clearance 3.622 uL/min/mg protein High 0.82
hppb Human plasma protein binding (% unbound) 54.930 % High 0.82
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 56
kinase-selectivity-class ACVR2B,AXL,CDK9,EIF2AK3,GRK2,MAP2K6,TEK,TGFBR1 8
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.302 Moderate 0.65
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.416 High 0.82
mh-clint Mouse hepatocyte intrinsic clearance 2.094 High 0.82
mppb Mouse plasma protein binding (% unbound) 82.450 High 0.82
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.176 High 0.82
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 46.670 % High 0.82
rat-kpuu-brain Rat brain Kpuu 0.006 % Moderate 0.65
rh-clint Rat hepatocyte intrinsic clearance 1.982 uL/min/10^6 cells High 0.82
rh-fuinc Rat hepatocyte fraction unbound in incubation 91.550 % High 0.82
rppb Rat plasma protein binding (% unbound) 46.670 % High 0.82
solubility-dd Solubility at pH 7.4 in DMSO 820.352 uM High 0.82

Approvals:

DateAgencyCompanyOrphan
Nov. 9, 1976 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bronchiectasis 178.52 135.36 41 770 22289 90605347
Bone erosion 143.33 135.36 41 770 52980 90574656
Hypothyroidism 143.25 135.36 41 770 53086 90574550

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01CA13 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
BETA-LACTAM ANTIBACTERIALS, PENICILLINS
Penicillins with extended spectrum
ATC J01CR03 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
BETA-LACTAM ANTIBACTERIALS, PENICILLINS
Combinations of penicillins, incl. beta-lactamase inhibitors
FDA CS M0016152 Penicillins
FDA EPC N0000175497 Penicillin-class Antibacterial
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents
CHEBI has role CHEBI:36047 antibacterial drug

Related Drugs by ATC class:

J01CA Penicillins with extended spectrum 18 drugs
amoxicillinampicillinaspoxicillinazlocillinbacampicillincarbenicillincarindacillinepicillinhetacillinmecillinammetampicillinmezlocillin show all 18 →
J01CR Combinations of penicillins, incl. beta-lactamase inhibitors 4 drugs
amoxicillinampicillinpiperacillinsultamicillin

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Septicemia due to Escherichia coli indication 9323009
Bacterial septicemia indication 10001005 DOID:0040085
Infection of skin AND/OR subcutaneous tissue indication 19824006
Staphylococcal pneumonia indication 22754005
Pneumonia due to Pseudomonas indication 41381004
Pneumonia due to Escherichia coli indication 51530003
Bacterial pneumonia indication 53084003 DOID:874
Empyema of pleura indication 58554001 DOID:3798
Klebsiella cystitis indication 60867007
Urinary tract infectious disease indication 68566005
Haemophilus influenzae pneumonia indication 70036007
Infection due to Escherichia coli indication 71057007
Bacterial infection due to Serratia indication 71120004
Rhinoscleroma indication 72409005 DOID:11336
Abscess of lung indication 73452002 DOID:0060317
Salpingitis indication 88157006 DOID:5733
Pelvic abscess indication 111367007
Infectious disease of abdomen indication 128070006
Infection due to Enterobacteriaceae indication 128945009
Bacterial infection due to Klebsiella pneumoniae indication 186435004
Proteus pneumonia indication 195888009
Proteus septicemia indication 300986008
Escherichia coli urinary tract infection indication 301011002
Bacterial urinary infection indication 312124009
Infection due to Staphylococcus aureus indication 406602003
Aspiration pneumonia indication 422588002 DOID:3240
Osteomyelitis due to Staphylococcus aureus indication 428783003
Sepsis due to Staphylococcus aureus indication 448417001
Sepsis due to Pseudomonas indication 448813005
Sepsis due to Gram negative bacteria indication 449082003
Bacteroides Endometritis indication
Enterobacter Pneumonia indication
Skin and Skin Structure Pseudomonas Aeruginosa Infection indication
Skin and Skin Structure Providencia Infection indication
Staphylococcus Aureus Joint Infection indication
E. Coli Endometritis indication
Bacteroides Peritonitis indication
Staphylococcus Aureus Urinary Tract Infection indication
Pseudomonas Aeruginosa Urinary Tract Infection indication
Skin and Skin Structure Proteus Infection indication
Complicated Urinary Tract Infections indication
Skin and Skin Structure Morganella Morganii Infection indication
Klebsiella Pneumoniae Peritonitis indication
Morganella Septicemia indication
Enterobacter Endometritis indication
Serratia Urinary Tract Infection indication
E. Coli Peritonitis indication
Staphylococcus Endometritis indication
Inflammatory Disease of Female Pelvic Organs indication
Klebsiella Endometritis indication
Genitourinary Tract Infections indication
Citrobacter Urinary Tract Infection indication
Complicated Genitourinary Tract Infection indication
Providencia Septicemia indication
Pyrexia of unknown origin off-label use 7520000
Chronic purulent otitis media off-label use 38394007 DOID:14247
Cholangitis off-label use 82403002 DOID:9446
Infection of bone off-label use 111253001
Escherichia coli meningitis off-label use 192655005
Diverticulitis of gastrointestinal tract off-label use 271366000
Infectious disorder of joint off-label use 363162000
Abscess of brain off-label use 441806004
Pseudomonas Respiratory Tract Infection in Cystic Fibrosis off-label use
Diabetic Foot Infection off-label use
Pseudomonas Aeruginosa Meningitis off-label use
Kidney disease contraindication 90708001 DOID:557
Infectious mononucleosis contraindication 271558008 DOID:8568
Pseudomembranous enterocolitis contraindication 397683000




🐶 Veterinary Drug Use

SpeciesUseRelation
Horses Endometritis caused by beta-hemolytic streptococci Indication

🐶 Veterinary products

ProductApplicantIngredients
Ticillin Zoetis Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.79 acidic
pKa2 3.39 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Bacterial penicillin-binding protein Enzyme INHIBITOR CHEMBL CHEMBL
Penicillin-binding protein 1A Enzyme WOMBAT-PK

External reference:

IDSource
4019948 VUID
N0000148033 NUI
D02241 KEGG_DRUG
29457-07-6 SECONDARY_CAS_RN
4018409 VANDF
4019948 VANDF
C0040193 UMLSCUI
CHEBI:9587 CHEBI
XT8 PDB_CHEM_ID
CHEMBL1449 ChEMBL_ID
DB01607 DRUGBANK_ID
CHEMBL1200855 ChEMBL_ID
D013982 MESH_DESCRIPTOR_UI
36921 PUBCHEM_CID
10928 IUPHAR_LIGAND_ID
3406 INN_ID
F93UJX4SWT UNII
10591 RXNORM
5581 MMSL
d00121 MMSL
002708 NDDF
004838 NDDF
111119006 SNOMEDCT_US
1148001 SNOMEDCT_US
372577006 SNOMEDCT_US

Pharmaceutical products:

None