PMID- 1524896
OWN - NLM
STAT- MEDLINE
DCOM- 19921019
LR  - 20190718
IS  - 0959-8049 (Print)
IS  - 0959-8049 (Linking)
VI  - 28A
IP  - 4-5
DP  - 1992
TI  - Comparative antitumour activity of vinblastine-isoleucinate and related vinca 
      alkaloids in human tumour xenografts.
PG  - 767-73
AB  - The antitumour activity of the investigational agent vinblastine-isoleucinate 
      (V-LEU) was compared with vintriptol, another investigational agent of the same 
      series of vinblastine-23-oyl amino acid derivatives, and vinblastine, their 
      clinically active parent compound, in a panel of nine human tumour xenografts 
      growing subcutaneously in nude mice. Compounds were administered intravenously at 
      equitoxic doses twice weekly. As assessed by optimal tumour growth inhibition and 
      tumour growth delay, vinblastine, V-LEU and vintriptol exhibited antitumour 
      activity in 8/9, 7/9 and 4/7 human tumour xenografts, respectively. When growth 
      curves and numbers of complete remissions were compared, V-LEU was the most 
      active agent in two malignant melanoma lines (THXO and LOX p28) and two small 
      cell lung carcinoma lines tested (LXFS 538 and WX 322), whereas vinblastine was 
      more active against the two colorectal carcinomas (CXF 243 and CXF 280). Notably, 
      the non small cell lung carcinoma (NSCLC) line AHXOL was resistant to the three 
      agents. The results of this study suggest that V-LEU was as active as vinblastine 
      in most tumour lines, exhibiting superior antitumour activity in malignant 
      melanoma, SCLC and breast cancer lines. The decision to bring this compound into 
      clinical trial shall await further confirmation of these preclinical results and 
      the evaluation of its toxicity profile in relation to other vinca alkaloids.
FAU - Hendriks, H R
AU  - Hendriks HR
AD  - EORTC New Drug Development Office, Free University Hospital, Amsterdam, The 
      Netherlands.
FAU - Langdon, S
AU  - Langdon S
FAU - Berger, D P
AU  - Berger DP
FAU - Breistol, K
AU  - Breistol K
FAU - Fiebig, H H
AU  - Fiebig HH
FAU - Fodstad, O
AU  - Fodstad O
FAU - Schwartsmann, G
AU  - Schwartsmann G
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Eur J Cancer
JT  - European journal of cancer (Oxford, England : 1990)
JID - 9005373
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Vinca Alkaloids)
RN  - 04Y7590D77 (Isoleucine)
RN  - 5V9KLZ54CY (Vinblastine)
RN  - MUJ5BW9BWR (vinleucinol)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/adverse effects/*pharmacology
MH  - Body Weight/drug effects
MH  - Breast Neoplasms/drug therapy/pathology
MH  - Dose-Response Relationship, Drug
MH  - Female
MH  - Humans
MH  - Isoleucine/*analogs & derivatives/pharmacology
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Mice, Nude
MH  - Neoplasm Transplantation
MH  - Neoplasms, Experimental/*drug therapy/pathology
MH  - Transplantation, Heterologous
MH  - Vinblastine/*analogs & derivatives/metabolism/pharmacology
MH  - Vinca Alkaloids/adverse effects/*pharmacology
EDAT- 1992/01/01 00:00
MHDA- 1992/01/01 00:01
CRDT- 1992/01/01 00:00
PHST- 1992/01/01 00:00 [pubmed]
PHST- 1992/01/01 00:01 [medline]
PHST- 1992/01/01 00:00 [entrez]
AID - 0959-8049(92)90112-F [pii]
AID - 10.1016/0959-8049(92)90112-f [doi]
PST - ppublish
SO  - Eur J Cancer. 1992;28A(4-5):767-73. doi: 10.1016/0959-8049(92)90112-f.