Abstract: Rodent therapeutic models are provided containing at least human hepatocytes and at least one of human hematopoietic bone marrow cells and human cord blood. Such rodent therapeutic models can also be immunodeficient and/or contain human intestinal enzymes. These partially humanized rodent therapeutic models can have at least partially humanized bone marrow and a partially humanized liver. These rodent models include mice. The rodent models can be transplanted with one or more tumors, for example, xenotransplantation with a human tumor. Toxicological and efficacy trials of various therapies, for example, anti-cancer therapies, can be performed with these rodent therapeutic models. Oral administration of camptothecin can demonstrate increased toxicity in the humanized mice.

Abstract: Methods of preparing CPT-esters are described. The methods include using at least one acid in the esterification reactions or acylation reactions of camptothecins.

Abstract: Hydrated crystalline camptothecin esters, such as crystalline aliphatic ester hydrates of camptothecin, pharmaceutical compositions containing crystalline aliphatic ester hydrates of camptothecin, methods of treating a cancer or malignant tumor using the crystalline camptothecin ester hydrates and methods of making the same are described.

Abstract: Methods of preparing CPT-esters are described. The methods include using at least one acid in the esterification reactions or acylation reactions of camptothecins.

Abstract: Halo-alkyl esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment, are also described.

Abstract: Cascade esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment are also described.

Abstract: A method of treating specific forms of cancer with water-insoluble 20(S)-camptothecin compounds with the closed-lactone ring intact and/or derivatives thereof is disclosed. The method includes administering the compounds intramuscularly, orally and transdermally.

Abstract: Derivatives of camptothecin are disclosed and are represented by the general formula: wherein when R2 is H, R1 is a C2-C4 alkyl group, a C5-C15 alkyl group, a C3-C8 cycloalkyl group, a C2-C15 alkenyl group or a C2-C15 epoxy group; and when R2 is a nitro group, R1 is a C1-C15 alkyl group, a C2-C15 alkenyl group, a C3-C8 cycloalkyl group, or an expoxy group. Processes for making these derivatives and for using them in cancer treatment are also disclosed.

Abstract: Aromatic camptothecin ester compounds having the formula: are described as well as formulations containing the compounds. Methods of treating cancer and/or tumors are also disclosed.

Abstract: Derivatives of camptothecin as represented by the general formula: are described, wherein when R1 is H, R. is a C2-C4 alkyl group, a C6-C15 alkyl group, a C3-C8 cycloalkyl group, a C2-C15 alkenyl group or a C2-C15 epoxy group; and when R2 is a nitro group or an amino group, R1 is a C1-C15 alkyl group, a C1-C15 alkenyl group, a C3-C8 cycloalkyl group, or an epoxy group. Liposomal prodrugs including these specific derivatives of camptothecin restrained by a liposomal delivery system are also described. Processes for making these prodrugs and for using them in cancer treatment are also disclosed.

Abstract: A method of treating specific forms of cancer with water-insoluble 20(S)-camptothecin compounds with the closed-lactone ring intact and/or derivatives thereof is disclosed. The method includes administering the compounds intramuscularly, orally and transdermally.

Abstract: Aromatic camptothecin ester compounds having the formula: are described as well as formulations containing the compounds. Methods of treating cancer and/or tumors are also disclosed.

Abstract: Derivatives of camptothecin are disclosed and are represented by the general formula: wherein when R2 is H, R1 is a C2-C4 alkyl group, a C6-C15 alkyl group, a C3-C8 cycloalkyl group, a C2-C15 alkenyl group or a C2-C15 epoxy group; and when R2 is a nitro group, R1 is a C1-C15 alkyl group, a C2-C5 alkenyl group, a C3-C8 cycloalkyl group, or an epoxy group. Processes for making these derivatives and for using them in cancer treatment are also disclosed.

Abstract: A method of treating specific forms of cancer with water-insoluble 20(S)-camptothecin compounds with the closed-lactone ring intact and/or derivatives thereof is disclosed. The method includes administering the compounds intramuscularly, orally and transdermally.

Abstract: Methods for purifying 20(S)-camptothecin are described. The 20(S)-camptothecin in purified form is useful in the treatment of cancer.

Abstract: Derivatives of camptothecin are disclosed and are represented by the general formula: ##STR1## wherein when R.sub.2 is H, R.sub.1 is a C.sub.2 -C.sub.4 alkyl group, a C.sub.6 -C.sub.15 alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group, a C.sub.2 -C.sub.15 alkenyl group or a C.sub.2 -C.sub.15 epoxy group; and when R.sub.2 is a nitro group, R.sub.1 is a C.sub.1 -C.sub.15 alkl group, a C.sub.2 -C.sub.15 alkenyl group, a C.sub.3 -C.sub.8 cycloalkyl group, or an epoxy group. Processes for making these derivatives and for using them in cancer treatment are also disclosed.

Abstract: Methods for purifying 20(S)-camptothecin are described. The 20(S)-camptothecin in purified form is useful in the treatment of cancer.

Abstract: Liposomal prodrugs include specific derivatives of camptothecin restrained by a liposomal delivery system. The derivatives of camptothecin are represented by the general formula: ##STR1## wherein when R.sub.2 is H, R.sub.1 is a C.sub.2 -C.sub.4 alkyl group, a C.sub.6 -C.sub.15 alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group, a C.sub.2 -C.sub.15 alkenyl group or a C.sub.2 -C.sub.15 epoxy group; and when R.sub.2 is a nitro group, R.sub.1 is a C.sub.1 -C.sub.15 alkyl group, a C.sub.2 -C.sub.15 alkenyl group, a C.sub.3 -C.sub.8 cycloalkyl group, or an epoxy group. Processes for making these prodrugs and for using them in cancer treatment are also disclosed.

Abstract: A method of treating human pancreatic cancer with water-insoluble 20(S)-camptothecin compounds with the closed-lactone ring intact and/or derivatives thereof is disclosed. The method includes preferably administering the compounds intramuscularly, orally, and transdermally.

Abstract: A method is disclosed for the preparation of 9-nitrocamptothecin which involves reacting 20-camptothecin with at least one inorganic nitrate salt and at least one acid effective in catalyzing the formation of a nitronium ion, where the reaction occurs at a temperature and for a time sufficient to form the 9-nitrocamptothecin. Also, methods of further purifying the 9-nitrocamptothecin by column chromatography or by reprecipitation is also disclosed.