Page last updated: 2024-11-11

cgp 48664

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

Description

4-amidinoindan-1-one 2'-amidinohydrazone: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9576789
CHEMBL ID1202793
CHEMBL ID65789
SCHEMBL ID19379381
MeSH IDM0219593

Synonyms (31)

Synonym
sardomozide chloride
CHEMBL1202793 ,
4-amidinoindan-1-one-2'-amidinohydrazone
4-aiah
hydrazinecarboximidamide, 2-(4-(aminoiminomethyl)-2,3-dihydro-1h-inden-1-ylidene)-
cgp 48664
sam 486a
sam486a
(1e)-1-(carbamimidoylhydrazono)indane-4-carboxamidine
cgp-48664
cgp-48664a
urea azine with 1-oxo-4-indancarboxamidine
4-amidinoindan-1-one 2'-amidinohydrazone
CHEMBL65789
AKOS016004846
AKOS016000728
bdbm50368644
unii-ceb05s0b9i
ceb05s0b9i ,
sardomozide [inn]
4-(aminoiminomethyl)-2,3-dihydro-1h-inden-1-one-diaminomethylenehydrazone
(e)-2-(4-carbamimidoyl-2,3-dihydro-1h-inden-1-ylidene)hydrazinecarboximidamide
(e)-1-((diaminomethylene)hydrazono)-2,3-dihydro-1h-indene-4-carboximidamide
(2e)-2-(4-carbamimidoyl-2,3-dihydro-1h-inden-1-ylidene)hydrazinecarboximidamide
SCHEMBL19379381
HY-13746
CS-0007772
(1e)-1-(diaminomethylidenehydrazinylidene)-2,3-dihydroindene-4-carboximidamide
4-amidinoindan-1-one 2/'-amidinohydrazone
A926062
AKOS040737423

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" SAM486A plasma concentrations were measured during the first cycle for pharmacokinetic and pharmacodynamic evaluations."( A phase I and pharmacokinetic study of SAM486A, a novel polyamine biosynthesis inhibitor, administered on a daily-times-five every-three-week schedule in patients with Advanced solid malignancies.
Barbet, NC; Capdeville, R; Choi, L; Clark, GM; Eckhardt, SG; Gan, G; Hammond, LA; Hidalgo, M; Linnartz, R; Moczygemba, J; Porter, CW; Rowinsky, EK; Siu, LL; Sklenar, IT; Von Hoff, DD; Weiss, GR, 2002
)
0.31
" Pharmacokinetic analyses demonstrated a rapid initial decrease in plasma drug concentrations at the end of infusion, followed by a long terminal elimination phase with a mean (+/- SD) terminal elimination half-life of 65."( A phase I and pharmacokinetic study of SAM486A, a novel polyamine biosynthesis inhibitor, administered on a daily-times-five every-three-week schedule in patients with Advanced solid malignancies.
Barbet, NC; Capdeville, R; Choi, L; Clark, GM; Eckhardt, SG; Gan, G; Hammond, LA; Hidalgo, M; Linnartz, R; Moczygemba, J; Porter, CW; Rowinsky, EK; Siu, LL; Sklenar, IT; Von Hoff, DD; Weiss, GR, 2002
)
0.31
" Pharmacodynamic assessment of tumoral tissues in 1 study patient demonstrated changes in the levels of polyamines and their biosynthetic enzymes consistent with SAMDC inhibition."( A phase I and pharmacokinetic study of SAM486A, a novel polyamine biosynthesis inhibitor, administered on a daily-times-five every-three-week schedule in patients with Advanced solid malignancies.
Barbet, NC; Capdeville, R; Choi, L; Clark, GM; Eckhardt, SG; Gan, G; Hammond, LA; Hidalgo, M; Linnartz, R; Moczygemba, J; Porter, CW; Rowinsky, EK; Siu, LL; Sklenar, IT; Von Hoff, DD; Weiss, GR, 2002
)
0.31

Compound-Compound Interactions

ExcerptReferenceRelevance
"The purpose of our study was to determine the maximum-tolerated dose, dose-limiting toxicity, safety profile, and pharmacokinetics of the polyamine synthesis inhibitor SAM486A given in combination with 5-fluorouracil/leucovorin (5-FU/LV) in cancer patients."( Phase I and pharmacokinetic study of the polyamine synthesis inhibitor SAM486A in combination with 5-fluorouracil/leucovorin in metastatic colorectal cancer.
Bootle, D; Bridgewater, J; Choi, L; de Bruijn, P; Eskens, FA; Ledermann, JA; Mueller, C; Planting, AS; Sklenar, I; Sparreboom, A; van Zuylen, L; Verweij, J, 2004
)
0.32
"The novel molecular agent SAM486A is tolerable and safe in combination with a standard 5-FU regimen in patients with advanced colorectal cancer."( Phase I and pharmacokinetic study of the polyamine synthesis inhibitor SAM486A in combination with 5-fluorouracil/leucovorin in metastatic colorectal cancer.
Bootle, D; Bridgewater, J; Choi, L; de Bruijn, P; Eskens, FA; Ledermann, JA; Mueller, C; Planting, AS; Sklenar, I; Sparreboom, A; van Zuylen, L; Verweij, J, 2004
)
0.32
" However, drug combination therapies expected to potentiate the effects of these drugs have yet to be systematically pursued."( The role of polyamines in human cancer: prospects for drug combination therapies.
Bachmann, AS, 2004
)
0.32

Dosage Studied

ExcerptRelevanceReference
" Although the three sublines were 2- to 10-fold less sensitive than the parent line to classical MDR-type agents, they were found in dose-response studies to be significantly more sensitive to DENSPM than the parent line."( Collateral sensitivity of human melanoma multidrug-resistant variants to the polyamine analogue, N1,N11-diethylnorspermine.
Bergeron, RJ; Ganis, B; Kramer, DL; Porter, CW; Rustum, Y; Wrzosek, C, 1994
)
0.29
" A dosing regimen of four weekly infusions followed by 2 weeks off therapy was studied."( Phase I and pharmacological study of weekly administration of the polyamine synthesis inhibitor SAM 486A (CGP 48 664) in patients with solid tumors. European Organization for Research and Treatment of Cancer Early Clinical Studies Group.
Barbet, NC; Bruntsch, U; Capdeville, R; Choi, L; Denis, LJ; Eskens, FA; Greim, GA; Hanauske, AR; Muskiet, FA; Planting, AS; van Zuylen, C; Verweij, J; Wanders, J; Wolff, I, 2000
)
0.31
" Treatment of cells with a second inhibitor of polyamine biosynthesis, the S-adenosylmethionine decarboxylase (SAMDC) inhibitor SAM486A, also resulted in a dosage dependent decrease in meprin alpha and MMP-7 mRNA."( Inhibitors of polyamine biosynthesis decrease the expression of the metalloproteases meprin alpha and MMP-7 in hormone-independent human breast cancer cells.
Bond, JS; Manni, A; Matters, GL, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's27 (52.94)18.2507
2000's22 (43.14)29.6817
2010's1 (1.96)24.3611
2020's1 (1.96)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (13.46%)5.53%
Reviews1 (1.92%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other44 (84.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]