Alkyllysophospholipid in Cancer Therapy

Effect of a Lysolecithin Analogue on Nonspecific Resistance to Infection of Mice

“…ET-18-OCH3 also has an effect on tumour growth in mice (Munder et al, 1981). The tumoricidal activity of the lysolecithin analogue may be explained by extracellular killing of the tumour cells either by macrophages or by polymorphonuclear leukocytes.…”

“…Accumulation of this potentially harmful compound has been observed after its injection into mice, or after incubation of macrophages in vitro, with immunological adjuvants like Freund's complete adjuvant. It was therefore postulated that the increased formation of LPC by an adjuvant-activated phospholipase A of macrophages might explain the mechanism of adjuvant activity in general Munder et al, 1970Munder et al, , 1979Munder et al, , 1981Munder et al, and 1983. If this is true LPC should act as an adjuvant itself, and this was found to be so.…”

Phase II Study of Ilmofosine in Patients with Malignant Melanoma

“…INN) is a synthetic 1-S-thioether alkyllysophospholipid derivative with the chemical formula 1-hexadecyl-mercapto-2-methoxymethyl-rac-glycero-3-phosphocholine. This new thioether phospholipid has been shown to possess antineoplastic, antimetastatic, anti-invasive and immunomodulating properties in several tumor models [1][2][3][4][5][6]. The antitumor activity of the alkyllysophospholipids has been explained by a direct and selective cytotoxic action on neo plastic cells and by the generation of immunocompetent cells of the monocyte-macrophage lineage in vitro and in vivo [7,8], In addition, differentiation induction in human and murine myeloid leukemia cells has been observed [9], The molecular mechanism of the direct antineoplastic effect of these com pounds is related to a possibly specific interference with the phospholipid metabolism of the tumor cells [3,10,11], In a phase I study the tolerability of orally administered ilmo fosine was investigated [12].…”

Influence of the Alkyllysophospholipid ET-18-OCH₃ on Methylnitrosourea-induced Rat Mammary Carcinomas

“…To this category belongs the class of alkylly sophospholipids which are derived by etherification of natural lysophospholipids with long-chain fatty acids [2,11]. Unlike normal cells, some tum or cells are incapable o f cleaving the Sn 1 ether bond [3,19] and are thus unable to prevent the inhibition of membrane-associated fatty acid metabolism induced by these compounds.…”

“…Alkyllysophospholipids have been shown to be ef fective against tum or cells in vitro [1,18] as well as against transplantable tumors [19] and possibly against hum an tum ors [4]. The latter results must be interpreted with some reservation because they were obtained in a phase I study.…”