Abstract: A pharmaceutical composition is provided having particles of a physical mixture that contain at least one 20-camptothecin or a derivative thereof, at least one surfactant, at least one stabilizer, and at least one diluent. The particles have a mean particle size of less than about 2500 nm. The pharmaceutical composition can be nano- or micro-sized particles containing the 20-camptothecin esters or derivatives thereof as part of a physical mixture, which can provide the active compound in a water-soluble/dispersible, bioavailable form. The particles can be used as an oral pharmaceutical composition which comprises the nano- or micro-sized form of 20-camptothecin esters or derivatives, such as in an oral suspension (e.g., an aqueous suspension), or capsules, or caplets. The pharmaceutical composition can be used in the treatment of a cancer or malignant tumor in a patient by oral administration thereof in a therapeutically effective amount.

Abstract: A pharmaceutical composition is provided having particles of a physical mixture that contain at least one 20-camptothecin or a derivative thereof, at least one surfactant, at least one stabilizer, and at least one diluent. The particles have a mean particle size of less than about 2500 nm. The pharmaceutical composition can be nano- or micro-sized particles containing the 20-camptothecin esters or derivatives thereof as part of a physical mixture, which can provide the active compound in a water-soluble/dispersible, bioavailable form. The particles can be used as an oral pharmaceutical composition which comprises the nano- or micro-sized form of 20-camptothecin esters or derivatives, such as in an oral suspension (e.g., an aqueous suspension), or capsules, or caplets. The pharmaceutical composition can be used in the treatment of a cancer or malignant tumor in a patient by oral administration thereof in a therapeutically effective amount.

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

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

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: Aromatic camptothecin ester compounds having the formula: 1

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: Derivatives of camptothecin are disclosed and are represented by the general formula: 1

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: 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: 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 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.