laromustine: has antineoplastic activity
ID Source | ID |
---|---|
PubMed CID | 3081349 |
CHEMBL ID | 167691 |
SCHEMBL ID | 2416976 |
MeSH ID | M0535286 |
Synonym |
---|
unii-14j2g0u3nq |
14j2g0u3nq , |
2'-(2-chloroethyl)-n-methyl-1',2'-bis(methylsulfonyl)carbamohydrazide |
nsc 734246 |
laromustine [usan:inn] |
101m |
onrigin |
vnp-40101m |
laromustine |
cloretazine |
methanesulfonic acid, 1-(2-chloroethyl)-2-((methylamino)carbonyl)-2-(methylsulfonyl)hydrazide |
vnp 40101m |
vnp40101m |
1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[(methylamino) carbonyl]hydrazine |
173424-77-6 |
nsc-734246 |
nsc734246 |
1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-((2-methylamino)carbonyl)hydrazine |
D08939 |
laromustine (usan) |
1-[2-chloroethyl(methylsulfonyl)amino]-3-methyl-1-methylsulfonylurea |
laromustin |
CHEMBL167691 |
DB05817 |
laromustine [mi] |
1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-((methylamino)carbonyl)hydrazine |
laromustine [usan] |
laromustine [mart.] |
laromustine [who-dd] |
2-(2-chloroethyl)-n-methyl-1,2-bis(methylsulfonyl)hydrazinecarboxamide |
laromustine [inn] |
PVCULFYROUOVGJ-UHFFFAOYSA-N |
SCHEMBL2416976 |
DTXSID30169614 |
Q26841309 |
Laromustine is a prodrug that yields a chloroethylating compound and a carbamoylating compound. It is a sulfonylhdrazine alkylator with significant antileukemia activity.
Excerpt | Reference | Relevance |
---|---|---|
"Laromustine is a prodrug that yields a chloroethylating compound (VNP-4090-CE) and a carbamoylating compound (methyl isocyanate)." | ( Laromustine, a sulfonyl hydrolyzing alkylating prodrug for cancer therapy. Pigneux, A, 2009) | 2.52 |
"Laromustine is a sulfonylhdrazine alkylator with significant antileukemia activity. " | ( Phase 3 randomized, placebo-controlled, double-blind study of high-dose continuous infusion cytarabine alone or with laromustine (VNP40101M) in patients with acute myeloid leukemia in first relapse. Albitar, M; Boskovic, D; Brandwein, J; Cahill, A; DeAngelo, D; Giles, F; Kell, J; O'Brien, S; Pigneux, A; Robak, T; Seiter, K; Staib, P; Stock, W; Stuart, R; Tallman, M; Thomas, X; Vey, N, 2009) | 2 |
Laromustine has significant activity in both older patients with previously untreated acute myeloid leukemia or high-risk myelodysplastic syndrome. It has limited extramedullary toxicity.
Excerpt | Reference | Relevance |
---|---|---|
"Laromustine has limited extramedullary toxicity." | ( Laromustine (cloretazine). Giles, F; Vey, N, 2010) | 2.52 |
"Laromustine has significant activity in AML. " | ( Laromustine (cloretazine). Giles, F; Vey, N, 2010) | 3.25 |
"Laromustine has significant activity in both older patients with previously untreated acute myeloid leukemia or high-risk myelodysplastic syndrome, including those with very poor-risk disease, and in patients with relapsed disease." | ( Clinical activity of laromustine (Onrigin™) in hematologic malignancies. Alvarado, Y; Giles, FJ; Kelly, KR; Swords, R, 2009) | 1.39 |
Laromustine is a novel sulfonylhydrazine alkylating agent with significant antileukaemic activity, alone, or combined with cytarabine or daunorubicin.
Excerpt | Relevance | Reference |
---|---|---|
" Although significant activity was seen, safety and optimal dosing in combination regimen remain to be established and are now being investigated." | ( Laromustine (cloretazine). Giles, F; Vey, N, 2010) | 1.8 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID110613 | Average percent change in body weight from onset to termination of therapy at dose 10(mg/kg) | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
AID733208 | Cytotoxicity against human DU145 cells expressing AGT after 4 to 24 hrs by clonogenic assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells. |
AID733210 | Cytotoxicity against mouse AGT negative EMT6 cells under aerobic conditions after 4 to 24 hrs by clonogenic assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells. |
AID733205 | Cytotoxicity against human DU145 cells expressing AGT at 10 to 80 uM after 4 hrs by clonogenic assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells. |
AID110615 | Average percent change in body weight from onset to termination of therapy at dose 15(mg/kg) | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
AID733204 | Binding affinity to mouse L1210 cell DNA assessed as DNA cross-linking activity at 10 to 50 uM using H33258 dye by rapid DNA renaturation assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells. |
AID121746 | %60 day survivors were determined for the compound as the mouse surviving after the 60 day treatment at dose 5 mg/kg | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
AID120019 | Average survival time of treated /control mice*100 was determined at a daily dose of 5 mg/kg | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
AID733201 | Cytotoxicity against human DU145 cells expressing AGT after 4 to 24 hrs by clonogenic assay in presence of 100 uM of AGT inhibitor O6-BG | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Chloroethylating and methylating dual function antineoplastic agents display superior cytotoxicity against repair proficient tumor cells. |
AID121740 | %60 day survivors were determined for the compound as the mouse surviving after the 60 day treatment at dose 10 mg/kg | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
AID121742 | %60 day survivors were determined for the compound as the mouse surviving after the 60 day treatment at dose 15 mg/kg | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
AID110619 | Average percent change in body weight from onset to termination of therapy at dose 5(mg/kg) | 1996 | Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3 | Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)- hydrazines. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (1.89) | 18.2507 |
2000's | 32 (60.38) | 29.6817 |
2010's | 20 (37.74) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.94) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 10 (18.87%) | 5.53% |
Reviews | 7 (13.21%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 36 (67.92%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |