Page last updated: 2024-11-11

tasidotin

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

Description

tasidotin: an antimitotic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9895066
CHEMBL ID2111109
SCHEMBL ID30068
MeSH IDM0490038

Synonyms (13)

Synonym
unii-05g07285dk
tasidotin [inn]
05g07285dk ,
tasidotin
192658-64-3
SCHEMBL30068
tasidotin [who-dd]
CHEMBL2111109
n,n-dimethyl-l-valyl-l-valyl-n-methyl-l-valyl-l-prolyl-lproline-t-butylamide
n-tert-butyl-1-{n-[2-(dimethylamino)-1-hydroxy-3-methylbutylidene]valyl-n-methylvalylprolyl}pyrrolidine-2-carboximidic acid
DTXSID80940930
Q27236114
(2s)-n-tert-butyl-1-[(2s)-1-[(2s)-2-[[(2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide

Research Excerpts

Pharmacokinetics

Tasidotin plasma concentrations declined biphasically with an effective half-life of < or =55 minutes, and approximately 11% was excreted unchanged in the urine. The pharmacokinetics of tasid nicotine were similar in plasma and tumors in LOX- and H460-implanted mice, indicating resistance was not due to pharmacokinetic factors.

ExcerptReferenceRelevance
" Pharmacokinetic samples were collected during the first course."( Phase I and pharmacokinetic study of the dolastatin-15 analogue tasidotin (ILX651) administered intravenously on days 1, 3, and 5 every 3 weeks in patients with advanced solid tumors.
Appleman, LJ; Bonate, PL; Cunningham, C; Eder, JP; Fram, RJ; Hammond, LA; Jekunen, A; Kirvan-Visovatti, M; Regan, E; Ruvuna, F; Ryan, DP; Vukelja, S; Weitman, S, 2005
)
0.57
" Tasidotin plasma concentrations declined biphasically with an effective half-life of < or =55 minutes, and approximately 11% was excreted unchanged in the urine."( Phase I and pharmacokinetic study of the dolastatin-15 analogue tasidotin (ILX651) administered intravenously on days 1, 3, and 5 every 3 weeks in patients with advanced solid tumors.
Appleman, LJ; Bonate, PL; Cunningham, C; Eder, JP; Fram, RJ; Hammond, LA; Jekunen, A; Kirvan-Visovatti, M; Regan, E; Ruvuna, F; Ryan, DP; Vukelja, S; Weitman, S, 2005
)
1.48
" Plasma and urine were sampled to characterize the pharmacokinetic behavior of tasidotin."( Phase I and pharmacokinetic study of tasidotin hydrochloride (ILX651), a third-generation dolastatin-15 analogue, administered weekly for 3 weeks every 28 days in patients with advanced solid tumors.
Bonate, PL; Chu, QS; DeBono, JS; Garrison, M; Hammond, LA; Jones, CB; McCreery, H; Mita, AC; Rowinsky, EK; Syed, S; Weiss, G; Weitman, S, 2006
)
0.83
" After tasidotin administration, the pharmacokinetics of tasidotin and tasidotin-C-carboxylate were similar in plasma and tumors in LOX- and H460-implanted mice, indicating the resistance was not due to pharmacokinetic factors."( Pharmacokinetics in mice implanted with xenografted tumors after intravenous administration of tasidotin (ILX651) or its carboxylate metabolite.
Beyerlein, D; Bonate, PL; Crawford, J; Krumbholz, R; Roth, S; Schmid, S, 2007
)
1.01
" Pharmacokinetic parameters were estimated using model-independent and model-dependent methods."( Plasma and cerebrospinal fluid pharmacokinetics of tasidotin (ILX-651) and its metabolites in non-human primates.
Berg, SL; Blaney, SM; Bonate, PL; Dauser, R; Gibson, BW; Kilburn, LB; McGuffey, L; Nuchtern, JG; Thompson, P, 2009
)
0.6
" The CSF AUC and half-life of tasidotin was 28 +/- 10 microM min and 96 +/- 40 min."( Plasma and cerebrospinal fluid pharmacokinetics of tasidotin (ILX-651) and its metabolites in non-human primates.
Berg, SL; Blaney, SM; Bonate, PL; Dauser, R; Gibson, BW; Kilburn, LB; McGuffey, L; Nuchtern, JG; Thompson, P, 2009
)
0.89
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (100.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.72

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.72 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (30.00%)5.53%
Reviews1 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]