Page last updated: 2024-11-06

balsalazide

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Description

Balsalazide is a prodrug that is converted to mesalazine (5-aminosalicylic acid, 5-ASA) in the colon. It is used to treat ulcerative colitis, a type of inflammatory bowel disease. Balsalazide is a derivative of salicylic acid. It is synthesized by reacting 5-aminosalicylic acid with a derivative of sulfasalazine. Balsalazide has anti-inflammatory effects that are thought to be due to its conversion to mesalazine, which inhibits the production of inflammatory mediators. It is studied because it is a targeted therapy for ulcerative colitis, meaning that it is specifically delivered to the colon, where it is needed. The localized delivery of mesalazine reduces the side effects associated with systemic administration of 5-ASA.'

balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond. [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 CID54585
CHEMBL ID1201346
CHEMBL ID1208641
CHEBI ID267413
CHEBI ID94605
SCHEMBL ID138311
SCHEMBL ID142548
SCHEMBL ID118300
SCHEMBL ID15841310
MeSH IDM0116205

Synonyms (83)

Synonym
BIDD:GT0772
HMS3394K19
balsalazidum [latin]
benzoic acid, 5-((4-(((2-carboxyethyl)amino)carbonyl)phenyl)azo)-2-hydroxy-, (e)-
balsalazida [spanish]
balsalazido [spanish]
balsalazide [inn:ban]
D07488
80573-04-2
balsalazide (inn)
MLS001424257
smr000469221
5-[4-(2-carboxy-ethylcarbamoyl)-phenylazo]-2-hydroxy-benzoic acid
(e)-5-((4-(((2-carboxyethyl)amino)carbonyl)phenyl)azo)-2-hydroxybenzoic acid
(e)-5-({p-[(2-carboxyethyl)carbamoyl]phenyl}azo)-2-salicylic acid
3-(2-{4-[(2-carboxyethyl)carbamoyl]phenyl}hydrazinylidene)-6-oxocyclohexa-1,4-diene-1-carboxylic acid
balsalazide
DB01014
NCGC00164634-01
5-[(e)-{4-[(2-carboxyethyl)carbamoyl]phenyl}diazenyl]-2-hydroxybenzoic acid
HMS2052K19
balsalazidum
CHEBI:267413 ,
balsalazida
balsalazido
A839951
3-[[4-(2-carboxyethylcarbamoyl)phenyl]hydrazono]-6-oxo-cyclohexa-1,4-diene-1-carboxylic acid
p80al8j7zp ,
unii-p80al8j7zp
CHEMBL1201346
dtxsid7040653 ,
tox21_112252
cas-80573-04-2
dtxcid5020653
CHEMBL1208641
(e)-5-((4-((2-carboxyethyl)carbamoyl)phenyl)diazenyl)-2-hydroxybenzoic acid
HMS2233C19
CCG-101140
FT-0602905
balsalazide [vandf]
balsalazide [mi]
balsalazide [who-dd]
balsalazide [inn]
5-((4-((2-carboxyethyl)carbamoyl)phenyl)diazenyl)-2-hydroxybenzoic acid
benzoic acid, 5-((4-(((2-carboxyethyl)amino)carbonyl)phenyl)azo)-2-hydroxy-
AKOS015892568
S4842
HMS3369E09
HY-B0667
AB01209737-01
5-(2-{4-[(2-carboxyethyl)carbamoyl]phenyl}diazen-1-yl)-2-hydroxybenzoic acid
SCHEMBL138311
SCHEMBL142548
SCHEMBL118300
NC00390
tox21_112252_1
NCGC00164634-02
KS-5215
IPOKCKJONYRRHP-UHFFFAOYSA-N
bacitracin zinc, antibiotic for culture media use only
Q-200671
SCHEMBL15841310
AC-8500
CHEBI:94605
(3e)-3-(2-{4-[(2-carboxyethyl)carbamoyl]phenyl}hydrazinylidene)-6-oxocyclohexa-1,4-diene-1-carboxylic acid
Q27166431
3-[[4-[(2-carboxyethylamino)-oxomethyl]phenyl]hydrazinylidene]-6-oxo-1-cyclohexa-1,4-dienecarboxylic acid
mfcd00868204
(e)-5-((4-(2-carboxyethylcarbamoyl)phenyl)diazenyl)-2-hydroxybenzoic acid
AS-17568
399030-81-0
Q347337
EN300-119538
5-[[4-(2-carboxyethylcarbamoyl)phenyl]diazenyl]-2-hydroxybenzoic acid
gtpl11569
F85019
(e)-5-[[[-4-(2-carboxyethyl)aminocarbonyl]phenyl]azo]-2-hydroxybenzoic acid
bdbm50565694
5-({4-[(2-carboxyethyl)carbamoyl]phenyl}diazenyl)-2-hydroxybenzoic acid
DTXSID50861027
benzoic acid, 5-[(1e)-2-[4-[[(2-carboxyethyl)amino]carbonyl]phenyl]diazenyl]-2-hydroxy-
balsalazide-d3disodiumsalt
Z2588038982

Research Excerpts

Overview

Balsalazide is a colon-specific prodrug of 5-aminosalicylate that is associated with a reduced risk of colon cancer in patients with ulcerative colitis. The drug releases mesalazine in the colon, thus exerting its multiple anti-inflammatory effects.

ExcerptReferenceRelevance
"Balsalazide is a colon-specific prodrug of 5-aminosalicylate that is associated with a reduced risk of colon cancer in patients with ulcerative colitis. "( Combined Parthenolide and Balsalazide Have Enhanced Antitumor Efficacy Through Blockade of NF-κB Activation.
Jeong, HJ; Kim, EM; Kim, IH; Kim, SH; Kim, SL; Kim, SW; Kim, YN; Lee, SO; Lee, ST; Liu, YC; Park, YR; Seo, SY, 2017
)
2.2
"Balsalazide is a 5-amino salicylic acid prodrug well-tolerated and effective in treating acute ulcerative colitis. "( Balsalazide plus high-potency probiotic preparation (VSL[sharp]3) in the treatment of acute mild-to-moderate ulcerative colitis and uncomplicated diverticulitis of the colon.
Tursi, A, 2008
)
3.23
"Balsalazide is an aminosalicylate prodrug that releases mesalazine in the colon, thus exerting its multiple anti-inflammatory effects in areas of colitis."( Balsalazide disodium for the treatment of ulcerative colitis.
Moss, AC; Patil, SA, 2008
)
2.51
"Balsalazide is a well tolerated and effective first-line therapeutic option for patients with ulcerative colitis, both for the treatment of active mild-to-moderate disease and as maintenance therapy to prevent disease relapse."( Balsalazide: a review of its therapeutic use in mild-to-moderate ulcerative colitis.
Goa, KL; Muijsers, RB, 2002
)
3.2
"Balsalazide is a novel azo-bonded 5-aminosalicylic acid treatment for mild-to-moderate ulcerative colitis. "( Balsalazide is superior to mesalamine in the time to improvement of signs and symptoms of acute mild-to-moderate ulcerative colitis.
Cross, A; Doty, P; Hanson, J; Hardi, R; Johanson, J; Johnson, LK; Koval, G; Pruitt, R; Riff, D; Safdi, M; Winston, B; Wruble, L, 2002
)
3.2
"Balsalazide is an effective and safe treatment for mild-to-moderate ulcerative colitis. "( Balsalazide is superior to mesalamine in the time to improvement of signs and symptoms of acute mild-to-moderate ulcerative colitis.
Cross, A; Doty, P; Hanson, J; Hardi, R; Johanson, J; Johnson, LK; Koval, G; Pruitt, R; Riff, D; Safdi, M; Winston, B; Wruble, L, 2002
)
3.2
"Balsalazide is a new-generation 5-ASA drug that yields a high concentration of active drug to the distal colon. "( Prevention of acute radiation-induced proctosigmoiditis by balsalazide: a randomized, double-blind, placebo controlled trial in prostate cancer patients.
Bettenhausen, D; Jahraus, CD; Malik, U; Sellitti, M; St Clair, WH, 2005
)
2.01
"Balsalazide is a mesalamine prodrug that is generally well tolerated and useful in the treatment of inflammatory bowel disease (IBD). "( Safety of balsalazide therapy in the treatment of inflammatory bowel disease.
Baker, DE, 2005
)
2.17
"Balsalazide is a novel mesalamine prodrug, activated by colonic bacteria."( Balsalazide is more effective and better tolerated than mesalamine in the treatment of acute ulcerative colitis. The Abacus Investigator Group.
Gibson, JA; Green, JR; Hodgson, HJ; Holdsworth, CD; Kerr, GD; Leicester, RJ; Lobo, AJ; Parkins, KJ; Taylor, MD, 1998
)
2.46
"Balsalazide is a prodrug of mesalazine which has an inert carrier molecule instead of the sulfapyridine moiety of sulfasalazine. "( Balsalazide.
Prakash, A; Spencer, CM, 1998
)
3.19
"Balsalazide is a 5-aminosalicylic acid (mesalazine) pro-drug which has an inert carrier molecule instead of the sulfapyridine moiety of sulfasalazine. "( Review article: balsalazide therapy in ulcerative colitis.
Ragunath, K; Williams, JG, 2001
)
2.1
"Balsalazide is a new 5-aminosalicylic acid (5-ASA) containing prodrug. "( Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses.
Brandes, JW; Ewald, U; Hämling, J; Howaldt, S; Koop, I; Krakamp, B; Kruis, W; Mönnikes, H; Pallant, D; Schreiber, S; Schütz, E; Stolte, M; Theuer, D, 2001
)
2.17
"Balsalazide is an azo-bonded pro-drug which also releases 5-aminosalicylic acid into the colon, but uses an inert carrier molecule."( A double-blind comparison of balsalazide, 6.75 g, and sulfasalazine, 3 g, as sole therapy in the management of ulcerative colitis.
Cann, PA; Giaffer, MH; Holdsworth, CD; Mansfield, JC; McKenna, D; Thornton, PC, 2002
)
1.33
"Balsalazide is a new innovative, mesalamine-containing prodrug that is activated by bacteria in the colon. "( A randomized, double blind, dose-response comparison of balsalazide (6.75 g), balsalazide (2.25 g), and mesalamine (2.4 g) in the treatment of active, mild-to-moderate ulcerative colitis.
Bell, JK; Johnson, LK; Koval, G; Levine, DS; Pruitt, R; Riff, DS; Sales, D; Wruble, L, 2002
)
2
"Balsalazide (BSZ) is a pro-drug which releases 5-aminosalicylic acid (5ASA) and 4-aminobenzoyl-beta-alanine (an inert carrier) in the colon of various species including man. "( Balsalazide in the maintenance treatment of patients with ulcerative colitis, a double-blind comparison with sulphasalazine.
Baron, JH; Barrison, IG; Lennard-Jones, JE; McIntyre, PB; Rodrigues, CA; Thornton, PC; Walker, JG, 1988
)
3.16

Effects

Balsalazide has been designed to deliver 5-aminosalicylic acid to the colon without the poor tolerability of sulfasalazine. The drug has been shown previously to be well tolerated and effective in the treatment of acute ulcerative colitis.

ExcerptReferenceRelevance
"Balsalazide has a unique delivery system in that 99% of ingested drug is delivered to and activated in the colon, a higher yield than all other oral agents currently available in this class."( Prevention of acute radiation-induced proctosigmoiditis by balsalazide: a randomized, double-blind, placebo controlled trial in prostate cancer patients.
Bettenhausen, D; Jahraus, CD; Malik, U; Sellitti, M; St Clair, WH, 2005
)
1.29
"Balsalazide has a unique delivery system in that 99% of ingested drug is delivered to and activated in the colon, a higher yield than all other oral agents currently available in this class."( Prevention of acute radiation-induced proctosigmoiditis by balsalazide: a randomized, double-blind, placebo controlled trial in prostate cancer patients.
Bettenhausen, D; Jahraus, CD; Malik, U; Sellitti, M; St Clair, WH, 2005
)
1.29
"Balsalazide has been designed to deliver 5-aminosalicylic acid to the colon without the poor tolerability of sulfasalazine."( A double-blind comparison of balsalazide, 6.75 g daily, and sulfasalazine, 3 g daily, in patients with newly diagnosed or relapsed active ulcerative colitis.
Gibson, JA; Green, JR; Kerr, GD; Mansfield, JC; Thornton, PC, 2002
)
1.33
"Balsalazide has been shown previously to be well tolerated and effective in the treatment of acute ulcerative colitis."( A randomized, double blind, dose-response comparison of balsalazide (6.75 g), balsalazide (2.25 g), and mesalamine (2.4 g) in the treatment of active, mild-to-moderate ulcerative colitis.
Bell, JK; Johnson, LK; Koval, G; Levine, DS; Pruitt, R; Riff, DS; Sales, D; Wruble, L, 2002
)
1.28

Toxicity

Adverse events requiring the withdrawal of therapy seem to occur less frequently with balsalazide, mesalamine, and olsalazine compared with sulfasalazine.

ExcerptReferenceRelevance
"To determine whether there is a difference in short-term adverse events in patients with ulcerative colitis treated with mesalazine, olsalazine or balsalazide."( Systematic review: short-term adverse effects of 5-aminosalicylic acid agents in the treatment of ulcerative colitis.
Bjorkman, D; Kane, SV; Loftus, EV, 2004
)
0.52
" Outcomes of interest were the frequencies of patients experiencing adverse events and those withdrawn due to adverse events."( Systematic review: short-term adverse effects of 5-aminosalicylic acid agents in the treatment of ulcerative colitis.
Bjorkman, D; Kane, SV; Loftus, EV, 2004
)
0.32
" sulfasalazine for active colitis showed significantly fewer patients with adverse events with mesalazine."( Systematic review: short-term adverse effects of 5-aminosalicylic acid agents in the treatment of ulcerative colitis.
Bjorkman, D; Kane, SV; Loftus, EV, 2004
)
0.32
"All three 5-aminosalicylic acid agents are safe in the short term."( Systematic review: short-term adverse effects of 5-aminosalicylic acid agents in the treatment of ulcerative colitis.
Bjorkman, D; Kane, SV; Loftus, EV, 2004
)
0.32
" Adverse events requiring the withdrawal of therapy seem to occur less frequently with balsalazide, mesalamine, and olsalazine compared with sulfasalazine."( The short- and long-term safety of 5-aminosalicylate products in the treatment of ulcerative colitis.
Baker, DE; Kane, S, 2004
)
0.55
" The most common adverse events reported were worsening of UC and headache; both were reported more often in the placebo group."( Safety and efficacy of a new 3.3 g b.i.d. tablet formulation in patients with mild-to-moderately-active ulcerative colitis: a multicenter, randomized, double-blind, placebo-controlled study.
Forbes, WP; Gordon, GL; Huang, S; Lamet, M; Mareya, S; Pruitt, R; Scherl, EJ; Shaw, A, 2009
)
0.35
" Adverse events and laboratory changes were monitored throughout the study."( Safety, efficacy, and pharmacokinetics of balsalazide in pediatric patients with mild-to-moderate active ulcerative colitis: results of a randomized, double-blind study.
Attard, TM; Bortey, E; Forbes, WP; Heyman, MB; Pieniaszek, HJ; Pohl, JF; Quiros, JA; Walker, K, 2009
)
0.62
" Adverse events were similar between the treatment groups, the most common being headache and abdominal pain."( Safety, efficacy, and pharmacokinetics of balsalazide in pediatric patients with mild-to-moderate active ulcerative colitis: results of a randomized, double-blind study.
Attard, TM; Bortey, E; Forbes, WP; Heyman, MB; Pieniaszek, HJ; Pohl, JF; Quiros, JA; Walker, K, 2009
)
0.62
" These adverse events appear to be caused by a hypersensitivity reaction and resolve after cessation of 5-ASA drugs."( Febrile pleuropericarditis, a potentially life-threatening adverse event of balsalazide--case report and literature review of the side effects of 5-aminosalicylates.
Coman, RM; Gjymishka, A; Glover, SC, 2014
)
0.63

Pharmacokinetics

The systemic absorption of 5-aminosalicylic acid from Asacol and balsalazide are comparable based upon plasma pharmacokinetic parameters and urinary excretion values.

ExcerptReferenceRelevance
" Sulphasalazine itself is poorly absorbed (3 to 12%) and its elimination half-life of about 5 to 10 hours is probably affected by the absorption process."( Clinical pharmacokinetics of sulphasalazine, its metabolites and other prodrugs of 5-aminosalicylic acid.
Klotz, U,
)
0.13
"Existing pharmacokinetic data are insufficient to determine whether a delayed-release formulation of mesalamine (Asacol) results in greater systemic exposure to 5-aminosalicylic acid and its major metabolite N-acetyl-5-aminosalicylic acid than a prodrug (balsalazide)."( Comparative pharmacokinetics of equimolar doses of 5-aminosalicylate administered as oral mesalamine (Asacol) and balsalazide: a randomized, single-dose, crossover study in healthy volunteers.
Buch, A; Hanauer, SB; Sandborn, WJ, 2004
)
0.71
"To determine the pharmacokinetic parameters of 5-aminosalicylic acid and N-acetyl-5-aminosalicylic acid from equimolar doses of 5-aminosalicylic acid administered as Asacol and balsalazide."( Comparative pharmacokinetics of equimolar doses of 5-aminosalicylate administered as oral mesalamine (Asacol) and balsalazide: a randomized, single-dose, crossover study in healthy volunteers.
Buch, A; Hanauer, SB; Sandborn, WJ, 2004
)
0.73
" Pharmacokinetic parameters assessed for 5-aminosalicylic acid and N-acetyl-5-aminosalicylic acid included: percentage of dose excreted in urine (A(e)%), area under the plasma concentration-time curve (AUCt(last)); and maximum plasma concentration (C(max))."( Comparative pharmacokinetics of equimolar doses of 5-aminosalicylate administered as oral mesalamine (Asacol) and balsalazide: a randomized, single-dose, crossover study in healthy volunteers.
Buch, A; Hanauer, SB; Sandborn, WJ, 2004
)
0.53
"The systemic absorption of 5-aminosalicylic acid and N-acetyl-5-aminosalicylic acid from Asacol and balsalazide are comparable based upon plasma pharmacokinetic parameters and urinary excretion values."( Comparative pharmacokinetics of equimolar doses of 5-aminosalicylate administered as oral mesalamine (Asacol) and balsalazide: a randomized, single-dose, crossover study in healthy volunteers.
Buch, A; Hanauer, SB; Sandborn, WJ, 2004
)
0.75
" Pharmacokinetic parameters for balsalazide, 5-aminosalicylic acid, and N-acetyl-5-aminosalicylic acid were determined at 2 weeks."( Safety, efficacy, and pharmacokinetics of balsalazide in pediatric patients with mild-to-moderate active ulcerative colitis: results of a randomized, double-blind study.
Attard, TM; Bortey, E; Forbes, WP; Heyman, MB; Pieniaszek, HJ; Pohl, JF; Quiros, JA; Walker, K, 2009
)
0.9

Bioavailability

ExcerptReferenceRelevance
" Sulphasalazine itself is poorly absorbed (3 to 12%) and its elimination half-life of about 5 to 10 hours is probably affected by the absorption process."( Clinical pharmacokinetics of sulphasalazine, its metabolites and other prodrugs of 5-aminosalicylic acid.
Klotz, U,
)
0.13
"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

Balsalazide is both highly effective in maintaining remission in ulcerative colitis and well tolerated in both conventional and high dosage. The dosage was 3 g/day versus mesalazine and 2 g/ day versus sulfasalazine.

ExcerptRelevanceReference
" The aim of this study was to determine the dose-response of balsalazide for efficacy and safety in active, mild-to-moderate ulcerative colitis and to compare this profile with that of mesalamine, pH-dependent, delayed-release tablets."( A randomized, double blind, dose-response comparison of balsalazide (6.75 g), balsalazide (2.25 g), and mesalamine (2.4 g) in the treatment of active, mild-to-moderate ulcerative colitis.
Bell, JK; Johnson, LK; Koval, G; Levine, DS; Pruitt, R; Riff, DS; Sales, D; Wruble, L, 2002
)
0.8
"6 g/day is recommended) and oral sulfasalazine 2 g/day (recommended dosage) in the prevention of relapse in ulcerative colitis in remission after 6 to 12 months of treatment; the balsalazide dosage was 3 g/day versus mesalazine and 2 g/day versus sulfasalazine."( Balsalazide: a review of its therapeutic use in mild-to-moderate ulcerative colitis.
Goa, KL; Muijsers, RB, 2002
)
1.95
" Mesalazine has been shown equivalent or superior to sulfasalazine, and superior to placebo, with a dose-response benefit, in inducing remission of acute disease."( Role of mesalazine in acute and long-term treatment of ulcerative colitis and its complications.
Schroeder, KW, 2002
)
0.31
"To assess the feasibility, safety and efficacy of patient-led dosing using balsalazide in the long-term treatment of ulcerative colitis."( Patient-led variable dosing with balsalazide as long-term therapy for maintenance in ulcerative colitis: a 3-year prospective observational study.
Gibson, JA; Green, JR; Kerr, GD; Swan, CH; Swarbrick, ET; Thornton, PC, 2004
)
0.83
"1 g tablet dosing regimen (6."( Safety and efficacy of a new 3.3 g b.i.d. tablet formulation in patients with mild-to-moderately-active ulcerative colitis: a multicenter, randomized, double-blind, placebo-controlled study.
Forbes, WP; Gordon, GL; Huang, S; Lamet, M; Mareya, S; Pruitt, R; Scherl, EJ; Shaw, A, 2009
)
0.35
" This new formulation with a reduced pill and dosing burden offers the potential to improve convenience and compliance in patients with active UC."( Safety and efficacy of a new 3.3 g b.i.d. tablet formulation in patients with mild-to-moderately-active ulcerative colitis: a multicenter, randomized, double-blind, placebo-controlled study.
Forbes, WP; Gordon, GL; Huang, S; Lamet, M; Mareya, S; Pruitt, R; Scherl, EJ; Shaw, A, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency89.12510.004023.8416100.0000AID485290
LuciferasePhotinus pyralis (common eastern firefly)Potency26.84720.007215.758889.3584AID1224835; AID624030
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.60320.006038.004119,952.5996AID1159521
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
AR proteinHomo sapiens (human)Potency0.00240.000221.22318,912.5098AID743042
EWS/FLI fusion proteinHomo sapiens (human)Potency17.85000.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency27.30940.023723.228263.5986AID743222; AID743241
Histone H2A.xCricetulus griseus (Chinese hamster)Potency39.07620.039147.5451146.8240AID1224845
histone deacetylase 9 isoform 3Homo sapiens (human)Potency25.11510.037617.082361.1927AID1259388
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC50 (µMol)4.46000.10003.38006.6000AID1742973; AID1742983; AID1771667; AID1863410; AID1885248
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)EC50 (µMol)8.80008.80008.80008.8000AID1863415
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
GTP biosynthetic processNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
UTP biosynthetic processNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
CTP biosynthetic processNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
lipid transportNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
nucleoside metabolic processNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
tryptophan metabolic processGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
fatty acid beta-oxidation using acyl-CoA dehydrogenaseGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
fatty-acyl-CoA biosynthetic processGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
protein deacetylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein deacetylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrion organizationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
regulation of ketone biosynthetic processNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
response to nutrient levelsNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein demalonylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
peptidyl-lysine demalonylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein desuccinylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
peptidyl-lysine desuccinylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein deglutarylationNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
epigenetic regulation of gene expressionNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
protein bindingNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
ATP bindingNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
metal ion bindingNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
cardiolipin bindingNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
nucleoside diphosphate kinase activityNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
glutaryl-CoA dehydrogenase activityGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
flavin adenine dinucleotide bindingGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
fatty-acyl-CoA bindingGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
zinc ion bindingNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
NAD-dependent protein lysine deacetylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein-malonyllysine demalonylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein-succinyllysine desuccinylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
protein-glutaryllysine deglutarylase activityNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
NAD+ bindingNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
mitochondrionNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
mitochondrial inner membraneNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
mitochondrial intermembrane spaceNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
mitochondrial matrixNucleoside diphosphate kinase, mitochondrialHomo sapiens (human)
mitochondrionGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
mitochondrial matrixGlutaryl-CoA dehydrogenase, mitochondrialHomo sapiens (human)
nucleusNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrionNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrial intermembrane spaceNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrial matrixNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
cytosolNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
mitochondrial matrixNAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (93)

Assay IDTitleYearJournalArticle
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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]
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]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1742974Inhibition of recombinant human SIRT5 at 50 uM using flour de lys succinyl as substrate in presence of NAD+ by fluorometric assay relative to control2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID1742975Inhibition of recombinant human SIRT1 (133 to 747 residues) expressed in Escherichia coli BL21(DE3) at 50 uM using ZMAL as substrate incubated for 4 hrs in presence of NAD+ followed by incubation with trypsin for 20 mins by trypsin-coupled assay based hom2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1863410Inhibition of recombinant human Sirt5 incubated for 1 hr by FLUOR DE LYS fluorometric microplate reader assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1742973Inhibition of recombinant human SIRT5 using flour de lys succinyl as substrate in presence of NAD+ by fluorometric assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID1863413Inhibition of recombinant Sirt3 (unknown origin) using ZMAL as fluorescence substrate at 50 uM incubated for 4.3 hrs by homogenous fluorescent deacetylase assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID1863411Inhibition of recombinant Sirt1 (unknown origin) using ZMAL as fluorescence substrate at 50 uM incubated for 4.3 hrs by homogenous fluorescent deacetylase assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
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]
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1863416Binding affinity to NME4 in human MCF7 cell lysate by pull down assay based LC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID1863409Cytotoxicity against human HeLa cells2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
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
AID1771667Inhibition of SIRT5 (unknown origin) assessed as reduction in GGQSLKFGKG formation using GGQSLK[succ]FGKG as substrate2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of new human Sirtuin 5 inhibitors by mimicking glutaryl-lysine substrates.
AID1742976Inhibition of recombinant human SIRT2 (25 to 389 residues) expressed in Escherichia coli BL21(DE3) at 50 uM using ZMAL as substrate incubated for 4 hrs in presence of NAD+ followed by incubation with trypsin for 20 mins by trypsin-coupled assay based homo2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID1863417Binding affinity to GCDH in human MCF7 cell lysate by pull down assay based LC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID1742977Inhibition of recombinant human SIRT3 (101 to 399 residues) expressed in Escherichia coli BL21(DE3) at 50 uM using ZMAL as substrate incubated for 4 hrs in presence of NAD+ followed by incubation with trypsin for 20 mins by trypsin-coupled assay based hom2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID1863414Inhibition of recombinant human Sirt5 at 50 uM incubated for 1 hr by FLUOR DE LYS fluorometric microplate reader assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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]
AID1742981Competitive inhibition of recombinant human SIRT5 assessed as substrate conversion at 50 uM using ZKsA as substrate in presence of increasing concentration of NAD+ by trypsin-coupled assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1863415Binding affinity to Sirt5 in human MCF7 cell lysate by pull down assay based LC-MS/MS analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
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]
AID1742983Inhibition of SIRT5 (unknown origin)2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' 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]
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1742982Competitive inhibition of recombinant human SIRT5 assessed as substrate conversion at 50 uM using increasing concentration of ZKsA as substrate in presence of NAD+ by trypsin-coupled assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1863418Inhibition of Sirt5 in human HeLa cells assessed as reduction on nano-fiber formation at 250 uM incubated for 90 mins by confocal laser scanning microscopic method2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID1885248Inhibition of SIRT5 (unknown origin) desuccinylation activity2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Therapeutic Potential and Activity Modulation of the Protein Lysine Deacylase Sirtuin 5.
AID1863419Inhibition of Sirt5 in human HeLa cells assessed as reduction on intracellular fluorescence at 250 uM incubated for 90 mins by confocal laser scanning microscopic method2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID1863412Inhibition of recombinant Sirt2 (unknown origin) using ZMAL as fluorescence substrate at 50 uM incubated for 4.3 hrs by homogenous fluorescent deacetylase assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Development of hetero-triaryls as a new chemotype for subtype-selective and potent Sirt5 inhibition.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID167806Concentration required to inhibit PAF-induced maximum aggregation by 50%2001Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (99)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (3.03)18.7374
1990's17 (17.17)18.2507
2000's50 (50.51)29.6817
2010's18 (18.18)24.3611
2020's11 (11.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.32

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index67.32 (24.57)
Research Supply Index4.81 (2.92)
Research Growth Index5.26 (4.65)
Search Engine Demand Index112.55 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (67.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (19.61%)5.53%
Reviews22 (21.57%)6.00%
Case Studies8 (7.84%)4.05%
Observational0 (0.00%)0.25%
Other52 (50.98%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Single-Dose Fasting In Vivo Bioequivalence Study of Balsalazide Disodium Capsules (750 mg; Mylan) and Colazal® Capsules (750 mg; Salix) in Healthy Volunteers [NCT00648531]Phase 180 participants (Actual)Interventional2004-05-31Completed
A Single Dose, Two-Period, Two-Treatment, Randomized Crossover Bioequivalency Study of 750 mg Balsalazide Capsules Under Fasting Conditions [NCT00618228]52 participants (Actual)Interventional2004-01-31Completed
A Single Dose, 2-Period, 2-Treatment, 2-Way Crossover Bioequivalency Study of Balsalazide Disodium 750 mg Capsules Under Fasting Conditions [NCT00618202]52 participants (Actual)Interventional2005-05-31Completed
Single-Dose Fed Bioequivalence Study of Balsalazide Disodium Capsules (750 mg; Mylan) and Colazal® Capsules (750 mg; Salix) in Healthy Volunteers [NCT00649480]Phase 160 participants (Actual)Interventional2007-01-31Completed
A Multicenter, Randomized, Double-Blind, Actively-Controlled Trial to Evaluate the Safety and Efficacy of a New Tablet Formulation and Dosing Regimen of Balsalazide Disodium 3.3 g Bid Versus Mesalamine (5-ASA) as Asacol® 0.8 g Tid in Mildly to Moderately [NCT00408174]Phase 3400 participants (Anticipated)Interventional2006-05-31Completed
A Multicenter, Open-label Trials to Evaluate the Long-term Safety and Tolerability of a New Balsalazide Disodium Tablet Formulation in Patients With Ulcerative Colitis [NCT00486031]Phase 3443 participants (Actual)Interventional2006-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00486031 (1) [back to overview]Incidence of Treatment Emergent AEs

Incidence of Treatment Emergent AEs

Incidence of treatment emergent adverse events (NCT00486031)
Timeframe: 24 Months

Interventionparticipants (Number)
Balsalazide Disodium273

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