Page last updated: 2024-12-06

pivampicillin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Pivampicillin is a penicillin-like antibiotic with a similar structure to ampicillin. It is the pivaloyloxymethyl ester of ampicillin. Pivampicillin is administered orally, and it is rapidly hydrolyzed in the body to ampicillin, which is then responsible for its antibacterial activity. It is used to treat a range of bacterial infections, including respiratory infections, urinary tract infections, and skin infections. Pivampicillin is particularly effective against gram-positive bacteria. The esterification of ampicillin with pivaloyloxymethyl provides better bioavailability and increased oral absorption compared to ampicillin. Due to its better absorption properties, pivampicillin is often preferred over ampicillin for the treatment of some infections, particularly in cases where higher concentrations of ampicillin are desired.'

Pivampicillin: Pivalate ester analog of AMPICILLIN. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

pivampicillin : A penicillanic acid ester that is the pivaloyloxymethyl ester of ampicillin. It is a prodrug of ampicillin. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID33478
CHEMBL ID3182343
CHEBI ID8255
SCHEMBL ID34182
MeSH IDM0016927

Synonyms (64)

Synonym
PRESTWICK2_001009
BPBIO1_001251
cas-33817-20-8
NCGC00016823-01
BSPBIO_001137
NCGC00179290-01
AB00513999
pivampicillin
33817-20-8
pivaloyloxymethyl ampicillinate
pivaloylampicillin
DB01604
ampicillin pivaloyloxymethyl ester
PRESTWICK3_001009
pivampicillin [inn:ban]
einecs 251-688-6
pivampicillinum [inn-latin]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-((aminophenylacetyl)amino)-3,3-dimethyl-7-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester, (2s-(2alpha,5alpha,6beta(s*)))-
pivampicilina [inn-spanish]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-, hydroxymethyl ester, pivalate (ester), d-(-)-
mk 191
pivampicilline [inn-french]
PRESTWICK1_001009
SPBIO_003018
PRESTWICK0_001009
pivampicilina
CHEBI:8255 ,
pivampicillinum
pivampicilline
[(2,2-dimethylpropanoyl)oxy]methyl 6beta-[(2r)-2-amino-2-phenylacetamido]-2,2-dimethylpenam-3alpha-carboxylate
2,2-dimethylpropanoyloxymethyl (2s,5r,6r)-6-[[(2r)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
pivampicillin (inn)
D08396
pondocillin (tn)
HMS1571I19
2,2-dimethylpropanoyloxymethyl (2s,5r,6r)-6-[(2-amino-2-phenylacetyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
HMS2098I19
dtxcid9025459
dtxsid1045459 ,
tox21_110631
unii-0hlm346ll7
0hlm346ll7 ,
[(2s,5r,6r)-6-[(2r)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carbonyloxy]methyl 2,2-dimethylpropanoate
mk-191
pivampicillin [mart.]
pivampicillin [who-dd]
pivampicillin [ep monograph]
hydroxymethyl d-(-)-6-(2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylate pivalate (ester)
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-((aminophenylacetyl)amino)-3,3-dimethyl-7-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester (2s-(2.alpha.,5.alpha.,6.beta.(s*)))-
pivampicillin [inn]
pivampicillin [mi]
CCG-221009
SCHEMBL34182
NCGC00179290-03
tox21_110631_1
CHEMBL3182343
{[(2s,5r,6r)-6-[(2r)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptan-2-yl]carbonyloxy}methyl 2,2-dimethylpropanoate
SR-01000872693-1
sr-01000872693
HMS3715I19
(2s,5r,6r)-pivaloyloxymethyl 6-((r)-2-amino-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
Q3122143
EN300-24137107
AKOS040744713

Research Excerpts

Overview

Pivampicillin is a prodrug which is widely used in Scandinavian countries for oral antibiotic therapy.

ExcerptReferenceRelevance
"Pivampicillin is a prodrug which is widely used in Scandinavian countries for oral antibiotic therapy. "( A follow-up study of birth outcome in users of pivampicillin during pregnancy.
Larsen, H; Møller, M; Nielsen, GL; Olsen, J; Schønheyder, HC; Sørensen, HT, 2000
)
2.01

Actions

ExcerptReferenceRelevance
"Pivampicillin can cause carnitine deficiency due to the pivalic acid side group."( Carnitine deficiency associated with long-term pivampicillin treatment: the effect of a replacement therapy regime.
Betteridge, DJ; Cooper, MB; Patel, S; Payne, JE; Rose, SJ; Stokes, TC, 1992
)
1.26

Treatment

Pivampicillin treatment was associated with formation and urinary excretion of pivaloylcarnitine. Administration of carnitine aided the elimination of pvalate as its carn itine ester. PivampICillin treatment results in inhibited oxidation of fats as metabolic fuel.

ExcerptReferenceRelevance
"Pivampicillin treatment was associated with formation and urinary excretion of pivaloylcarnitine and administration of carnitine aided the elimination of pivalate as its carnitine ester."( Carnitine administration ameliorates the changes in energy metabolism caused by short-term pivampicillin medication.
Kopcsányi, G; Masszi, G; Melegh, B; Molnár, D; Pap, M, 1997
)
1.24
"Pivampicillin treatment results in inhibited oxidation of fats as metabolic fuel. "( Carnitine administration ameliorates the changes in energy metabolism caused by short-term pivampicillin medication.
Kopcsányi, G; Masszi, G; Melegh, B; Molnár, D; Pap, M, 1997
)
1.96
"Pivampicillin treatment reduced the carnitine concentrations in the liver of the 48 hr fasted rat to about 1/2 of the controls after 6 days."( Reduced carnitine and ketogenesis in the pivampicillin treated rat.
Bøhmer, T; Diep, QN; Schjerven, L, 1992
)
1.27
"Pivampicillin treatment of seven children (five boys and two girls) for 7 days significantly reduced the amounts of total acid-soluble carnitine, free carnitine, and long-chain acylcarnitines and increased the amounts of acid-soluble acylcarnitine in plasma. "( Pivampicillin-promoted excretion of pivaloylcarnitine in humans.
Bieber, LL; Kerner, J; Melegh, B, 1987
)
3.16

Toxicity

ExcerptReferenceRelevance
" No adverse effects other than loose faeces and diarrhoea were detected."( Side effects of oral antimicrobial agents in the horse: a comparison of pivampicillin and trimethoprim/sulphadiazine.
Barneveld, A; Ensink, JM; Klein, WR; van Miert, AS; Vulto, AG, 1996
)
0.53

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic analysis was made according to a two-compartment open model."( Pharmacokinetics of ampicillin and its prodrugs bacampicillin and pivampicillin in man.
Boréus, LO; Ehrnebo, M; Nilsson, SO, 1979
)
0.5
" Base and hydrochloride of pivampicillin are equivalent with respect to pharmacokinetic behaviour."( [Studies on the pharmacokinetic equivalence of pivampicillin base and hydrochloride in capsules and tablets (author's transl)].
Bozler, G; Fedorcak, V; Mielenz, H, 1977
)
0.81

Compound-Compound Interactions

The results of three separate studies aimed at evaluating the efficacy of low-dose treatment with pivmecillinam alone, and in combination with pivampicillin are presented.

ExcerptReferenceRelevance
"The results of three separate studies aimed at evaluating the efficacy of long-term, low-dose treatment with pivmecillinam alone, and in combination with pivampicillin, in patients prone to recurrent bacteriuria, are presented."( Long-term, low-dose treatment with pivmecillinam alone and in combination with pivampicillin in patients prone to recurrent bacteriuria.
Barclay, RP; Mejlhede, A; Nilsson, LB, 1982
)
0.69
"3 patients with salmonella infections who continued to excrete salmonella in fecal samples for more than 6 months were treated with pivmecillinam alone or in combination with pivampicillin."( Treatment of Salmonella carriers with pivmecillinam alone or in combination with pivampicillin: experience with three patients.
Bruun, JN; Bøe, J; Digranes, A; Maeland, A, 1983
)
0.69

Bioavailability

Ampicillin, which binds to feedstuffs to a lesser extent, has a lower bioavailability than pivampicillin. The oral bioavailability of pivampsicillin was determined in the same foals at four ages.

ExcerptReferenceRelevance
" The bioavailability and urine concentration were also greater."( Ampicillin and pivampicillin in the treatment of urinary tract infection in children.
Eng, J; Meberg, A; Moe, OJ, 1977
)
0.61
"7 microgram/ml-h after ampicillin, reflecting the superior bioavailability of the ester form."( Oral absorption of pivampicillin and ampicillin in young children: cross-over study using equimolar doses of a suspension.
Pedersen-Bjergaard, L; Petersen, KE,
)
0.46
" The bioavailability of the esters bacampicillin (86 +/- 11%) and pivampicillin (92 +/- 18%) was significantly greater than that of ampicillin (62 +/- 17%); however, the difference between the esters was not statistically significant."( Pharmacokinetics of ampicillin and its prodrugs bacampicillin and pivampicillin in man.
Boréus, LO; Ehrnebo, M; Nilsson, SO, 1979
)
0.73
" Furthermore, bacampicillin had a higher absorption rate than all the other drugs, although there were statistically significant differences only versus ampicillin."( Pharmacokinetics of bacampicillin compared with those of ampicillin, pivampicillin, and amoxycillin.
Bergan, T; Magni, L; Sjövall, J, 1978
)
0.49
"The rates at which ampicillin, amoxycillin, metampicillin, hetacillin, and pivampicillin are absorbed from the bovine udder were compared, with the absorption rate of (14C)urea as reference."( Absorption of ampicillin derivatives from the bovine udder.
Ziv, G, 1976
)
0.49
" The (absolute) bioavailability of pivampicillin administered orally was 30."( Bioavailability of oral penicillins in the horse: a comparison of pivampicillin and amoxicillin.
Ensink, JM; Klarenbeek, A; Klein, WR; Mevius, DJ; Vulto, AG, 1992
)
0.8
" There were no significant differences between these three treatments in respect of the serum and bronchial secretion concentrations at the time of bronchoscopy, nor were there any significant differences in the peak serum level or total bioavailability of each regimen."( Penetration of ampicillin ('Pondocillin') and amoxycillin ('Imacillin') into bronchial secretions.
Hagstad, H, 1984
)
0.27
" The oral bioavailability of pivampicillin was determined in the same foals at four ages, ranging from 11 days to 4 months."( Oral bioavailability of pivampicillin in foals at different ages.
Barneveld, A; Ensink, JM; Klein, WR; van Miert, AS; Vulto, AG, 1994
)
0.89
" When bacampicillin and pivampicillin (two ampicillin prodrugs) were administered to horses, high oral bioavailability was obtained, and the use of prodrugs commands the need for further investigation."( Ampicillin and its congener prodrugs in the horse.
McKellar, QA; Sarasola, P,
)
0.44
"Absolute oral bioavailability was 31, 39, 23, and 2% for pivampicillin, bacampicillin, talampicillin, and ampicillin sodium, respectively."( Oral bioavailability and in vitro stability of pivampicillin, bacampicillin, talampicillin, and ampicillin in horses.
Ensink, JM; Fluitman, MA; Tukker, JJ; van Miert, AS; Vulto, AG; Winkel, MB, 1996
)
0.8
" Ampicillin, which binds to feedstuffs to a lesser extent, has a lower bioavailability than pivampicillin."( Bioavailability of pivampicillin and ampicillin trihydrate administered as an oral paste in horses.
Ensink, JM; Moi, A; Tukker, JJ; Vulto, AG, 1996
)
0.84
"Pivampicillin (PIVA), an acyloxymethylester of ampicillin, is thought to enhance the oral bioavailability of ampicillin because of its greater lipophilicity compared to that of ampicillin."( Accumulation and oriented transport of ampicillin in Caco-2 cells from its pivaloyloxymethylester prodrug, pivampicillin.
Chanteux, H; Mingeot-Leclercq, MP; Tulkens, PM; Van Bambeke, F, 2005
)
1.98
" The bioavailability of ampicillin, taken as the area under the serum curve, obtained with pivampicillin at a 250-mg ampicillin dose level was superior to that obtained with a 500-mg dose of ampicillin."( Clinical pharmacology of pivampicillin.
Kristensen, E; Nielsen, B; Roholt, K, 1974
)
0.78
" Pivampicillin was absorbed well in non-fasted horses with an oral bioavailability of 36%."( Pharmacokinetics in pulmonary epithelial lining fluid and plasma of ampicillin and pivampicillin administered to horses.
Baptiste, KE; Friis, C; Winther, L, 2012
)
1.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Pivampicillin was administered in half of the dosage of ampicillin. The resulting peak serum concentration was 65% higher and was achieved more rapidly. Of the 493 women in the study, 254 received dosed of 2 million IU of penicillin G intermuscularly.

ExcerptRelevanceReference
" Despite the fact that pivampicillin was administered in half of the dosage of ampicillin the resulting peak serum concentration was 65% higher and was achieved more rapidly."( Ampicillin and pivampicillin in the treatment of urinary tract infection in children.
Eng, J; Meberg, A; Moe, OJ, 1977
)
0.92
" Controls over a 15-weeks period showed that this dosage did prevent the development of syphilitic orchitis and reactivity to the quantitative FTA-ABS-test."( [The effect of pivampicillin and probenecid on experimental syphilis in rabbits].
Petzoldt, D, 1975
)
0.61
" The pivampicillin dosage was 700 mg twice a day and the erythromycin dosage 500 mg twice a day for seven days."( Pivampicillin compared with erythromycin for treating women with genital Chlamydia trachomatis infection.
Cramers, M; From, E; Kaspersen, P; Møller, BR, 1988
)
2.23
" Of the 493 women in the study, 254 received dosed of 2 million IU of penicillin G intermuscularly 1/2 hour before and 3 hours after the procedure, followed by 350 mg of pivampicillin 3 times daily for 4 days, and 239 women received corresponding doses of placebo."( Prophylactic antibiotics in first-trimester abortions: a clinical, controlled trial.
Andersen, JT; Dyring-Andersen, K; Hebjøorn, S; Heisterberg, L; Hejl, BL; Sonne-Holm, S, 1981
)
0.46
"The efficacy and tolerance of two different dosage regimens of pivampicillin was compared in 155 patients with acute sinusitis and in 56 patients with otitis media."( Treatment of sinusitis and otitis media with pivampicillin.
Christensen, CH; Hartmann, E, 1980
)
0.76
" To obtain the same ratio between ampicillin serum levels and MIC (minimum inhibitory concentration) in the pregnant as in the non-pregnant subject, a double dosage should be used."( Study of ampicillin levels in maternal serum, umbilical cord serum and amniotic fluid following administration of pivampicillin.
Hagen, AG; Jordheim, O, 1980
)
0.47
"The drugs were administered intragastrically to the horses at a dosage equimolar to 15 mg of ampicillin/kg of body weight."( Oral bioavailability and in vitro stability of pivampicillin, bacampicillin, talampicillin, and ampicillin in horses.
Ensink, JM; Fluitman, MA; Tukker, JJ; van Miert, AS; Vulto, AG; Winkel, MB, 1996
)
0.55
" Concentrations in TCF remained above the minimum inhibitory concentration of Streptococcus zooepidemicus for the proposed dosing intervals of 8, 12 and 24 h for ampicillin sodium, pivampicillin and procaine penicillin G respectively."( Distribution of penicillins into subcutaneous tissue chambers in ponies.
Barneveld, A; Ensink, JM; Klein, WR; Tukker, JJ; Van Miert, AS; Vulto, AG, 1996
)
0.49
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
penicillanic acid ester
pivaloyloxymethyl esterA acetal obtained from a carboxylic acid by replacement of the hydrogen attached to the carboxy group by a pivaloyloxymethyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.16550.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency10.59090.003041.611522,387.1992AID1159552
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
GVesicular stomatitis virusPotency27.54040.01238.964839.8107AID1645842
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency2.03710.001019.414170.9645AID743094
activating transcription factor 6Homo sapiens (human)Potency0.47720.143427.612159.8106AID1159516
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency23.914519.739145.978464.9432AID1159509
heat shock protein beta-1Homo sapiens (human)Potency33.48890.042027.378961.6448AID743210
Interferon betaHomo sapiens (human)Potency27.54040.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency27.54040.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (215)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990150 (69.77)18.7374
1990's42 (19.53)18.2507
2000's7 (3.26)29.6817
2010's10 (4.65)24.3611
2020's6 (2.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.50 (24.57)
Research Supply Index5.73 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index61.55 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials74 (31.90%)5.53%
Reviews7 (3.02%)6.00%
Case Studies12 (5.17%)4.05%
Observational0 (0.00%)0.25%
Other139 (59.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]