METHODS OF ADMINISTERING EPOTHILONE ANALOGS FOR THE TREATMENT OF CANCER

Formulating an epothilone analog (I) for parenteral administration, comprises: (A) dissolving the analog in tert-butanol and water; (B) primary drying at -10 - -40 EC; (C) secondary drying at 10 - 30 EC; and (D) packaging the lyophilized product in a first vial in combination with a second vial cont...

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Hauptverfasser: KRISHNASWAMY SRINIVAS RAGHAVAN, REBANTA BANDYOPADHYAY, ANDREA PANAGGIO, SAILESH AMILAL VARIA, TIMOTHY M. MALLOY
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creator KRISHNASWAMY SRINIVAS RAGHAVAN
REBANTA BANDYOPADHYAY
ANDREA PANAGGIO
SAILESH AMILAL VARIA
TIMOTHY M. MALLOY
description Formulating an epothilone analog (I) for parenteral administration, comprises: (A) dissolving the analog in tert-butanol and water; (B) primary drying at -10 - -40 EC; (C) secondary drying at 10 - 30 EC; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. Formulating an epothilone analog of formula (I) or their salt, solvate or hydrate for parenteral administration, comprises: (A) dissolving (I) in a mixture of tert-butanol (50 vol.%) in water to form a solution; (B) primary drying at -10 - -40 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours to form lyophilized product; (C) secondary drying the resultant lyophilized product at 10 - 30 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. [Image] Q : M-CH(R 7>)(CH 3) or CH=C(R 7>); M : O, S, NR 8> or CR 9>R 1> 0>; R 1> - R 5>, R 7> and R 1> 1> - R 1> 5>alkyl, aryl (both optionally substituted), H or heterocyclo; R 1>+R 2>cycloalkyl; R 6>alkyl, aryl, heterocyclo (all optionally substituted) or H; R 8>H, alkyl (optionally substituted), R 1> 1>C=O, R 1> 2>OC=O or R 1> 3>SO 2; and R 9> and R 1> 0>H, halo, alkyl (optionally substituted), aryl, heterocyclo, hydroxy, R 1> 4>C=O or R 1> 5>OC=O. Independent claims are also included for: (1) A pharmaceutical preparation (II) comprising, in separate vials, lyophilized (I) and its solvent such that when the contents of the vials are combined, the resulting solution contains (I) (2 - 4 mg/ml). The solvent mixture comprises a mixture of about equal parts by volume of dehydrated ethanol and the nonionic surfactant; (2) Process for forming a pharmaceutical composition for parenteral administration; (3) Treating a patient involving administering to the patient by intravenous injection the (II); (4) Treating cancer involving intravenously and orally administering (I); (5) A pharmaceutical composition (III) for parenteral administration comprising (I), dehydrated alcohol and non-ionic surfactant; (6) Method of treating cancer in a patient previously experiencing neurotoxicity involving intravenously administering the composition diluted in a parenteral diluent as a weekly infusion in dose of less than 200 mg/m 2>; (7) Treating cancer in a patient involving
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MALLOY</creatorcontrib><description>Formulating an epothilone analog (I) for parenteral administration, comprises: (A) dissolving the analog in tert-butanol and water; (B) primary drying at -10 - -40 EC; (C) secondary drying at 10 - 30 EC; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. Formulating an epothilone analog of formula (I) or their salt, solvate or hydrate for parenteral administration, comprises: (A) dissolving (I) in a mixture of tert-butanol (50 vol.%) in water to form a solution; (B) primary drying at -10 - -40 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours to form lyophilized product; (C) secondary drying the resultant lyophilized product at 10 - 30 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. [Image] Q : M-CH(R 7&gt;)(CH 3) or CH=C(R 7&gt;); M : O, S, NR 8&gt; or CR 9&gt;R 1&gt; 0&gt;; R 1&gt; - R 5&gt;, R 7&gt; and R 1&gt; 1&gt; - R 1&gt; 5&gt;alkyl, aryl (both optionally substituted), H or heterocyclo; R 1&gt;+R 2&gt;cycloalkyl; R 6&gt;alkyl, aryl, heterocyclo (all optionally substituted) or H; R 8&gt;H, alkyl (optionally substituted), R 1&gt; 1&gt;C=O, R 1&gt; 2&gt;OC=O or R 1&gt; 3&gt;SO 2; and R 9&gt; and R 1&gt; 0&gt;H, halo, alkyl (optionally substituted), aryl, heterocyclo, hydroxy, R 1&gt; 4&gt;C=O or R 1&gt; 5&gt;OC=O. Independent claims are also included for: (1) A pharmaceutical preparation (II) comprising, in separate vials, lyophilized (I) and its solvent such that when the contents of the vials are combined, the resulting solution contains (I) (2 - 4 mg/ml). The solvent mixture comprises a mixture of about equal parts by volume of dehydrated ethanol and the nonionic surfactant; (2) Process for forming a pharmaceutical composition for parenteral administration; (3) Treating a patient involving administering to the patient by intravenous injection the (II); (4) Treating cancer involving intravenously and orally administering (I); (5) A pharmaceutical composition (III) for parenteral administration comprising (I), dehydrated alcohol and non-ionic surfactant; (6) Method of treating cancer in a patient previously experiencing neurotoxicity involving intravenously administering the composition diluted in a parenteral diluent as a weekly infusion in dose of less than 200 mg/m 2&gt;; (7) Treating cancer in a patient involving intravenously administering to the patient the formulation in a parenteral diluent; (8) Treating cancer by reducing or avoiding neurotoxicity involving intravenously infusing (I) over a period of one hour to the patient; and (9) Method of treating cancer in human patient with a synthetic or semi-synthetic epothilone analog involving a four week dosing cycle where the cycle comprises 3 weeks of weekly intravenous administration and one week of oral administration of the analog. ACTIVITY : Cytostatic; Antitumor; Anti-HIV; Antiarthritic; Antiinflammatory; Vasotropic; Neuroprotective; Osteopathic; Virucide; Dermatological; Immunosuppressive; Antirheumatic; Nootropic; Antiparkinsonian; Antiallergic; Antidiabetic; Antipsoriatic; Antidepressant; Antianemic; Cerebroprotective; Antiarrhythmic; Antiarteriosclerotic; Cardiant. No biological data available. MECHANISM OF ACTION : Apoptosis modulator. 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MALLOY</creatorcontrib><title>METHODS OF ADMINISTERING EPOTHILONE ANALOGS FOR THE TREATMENT OF CANCER</title><description>Formulating an epothilone analog (I) for parenteral administration, comprises: (A) dissolving the analog in tert-butanol and water; (B) primary drying at -10 - -40 EC; (C) secondary drying at 10 - 30 EC; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. Formulating an epothilone analog of formula (I) or their salt, solvate or hydrate for parenteral administration, comprises: (A) dissolving (I) in a mixture of tert-butanol (50 vol.%) in water to form a solution; (B) primary drying at -10 - -40 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours to form lyophilized product; (C) secondary drying the resultant lyophilized product at 10 - 30 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. [Image] Q : M-CH(R 7&gt;)(CH 3) or CH=C(R 7&gt;); M : O, S, NR 8&gt; or CR 9&gt;R 1&gt; 0&gt;; R 1&gt; - R 5&gt;, R 7&gt; and R 1&gt; 1&gt; - R 1&gt; 5&gt;alkyl, aryl (both optionally substituted), H or heterocyclo; R 1&gt;+R 2&gt;cycloalkyl; R 6&gt;alkyl, aryl, heterocyclo (all optionally substituted) or H; R 8&gt;H, alkyl (optionally substituted), R 1&gt; 1&gt;C=O, R 1&gt; 2&gt;OC=O or R 1&gt; 3&gt;SO 2; and R 9&gt; and R 1&gt; 0&gt;H, halo, alkyl (optionally substituted), aryl, heterocyclo, hydroxy, R 1&gt; 4&gt;C=O or R 1&gt; 5&gt;OC=O. Independent claims are also included for: (1) A pharmaceutical preparation (II) comprising, in separate vials, lyophilized (I) and its solvent such that when the contents of the vials are combined, the resulting solution contains (I) (2 - 4 mg/ml). The solvent mixture comprises a mixture of about equal parts by volume of dehydrated ethanol and the nonionic surfactant; (2) Process for forming a pharmaceutical composition for parenteral administration; (3) Treating a patient involving administering to the patient by intravenous injection the (II); (4) Treating cancer involving intravenously and orally administering (I); (5) A pharmaceutical composition (III) for parenteral administration comprising (I), dehydrated alcohol and non-ionic surfactant; (6) Method of treating cancer in a patient previously experiencing neurotoxicity involving intravenously administering the composition diluted in a parenteral diluent as a weekly infusion in dose of less than 200 mg/m 2&gt;; (7) Treating cancer in a patient involving intravenously administering to the patient the formulation in a parenteral diluent; (8) Treating cancer by reducing or avoiding neurotoxicity involving intravenously infusing (I) over a period of one hour to the patient; and (9) Method of treating cancer in human patient with a synthetic or semi-synthetic epothilone analog involving a four week dosing cycle where the cycle comprises 3 weeks of weekly intravenous administration and one week of oral administration of the analog. ACTIVITY : Cytostatic; Antitumor; Anti-HIV; Antiarthritic; Antiinflammatory; Vasotropic; Neuroprotective; Osteopathic; Virucide; Dermatological; Immunosuppressive; Antirheumatic; Nootropic; Antiparkinsonian; Antiallergic; Antidiabetic; Antipsoriatic; Antidepressant; Antianemic; Cerebroprotective; Antiarrhythmic; Antiarteriosclerotic; Cardiant. No biological data available. MECHANISM OF ACTION : Apoptosis modulator. 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Formulating an epothilone analog of formula (I) or their salt, solvate or hydrate for parenteral administration, comprises: (A) dissolving (I) in a mixture of tert-butanol (50 vol.%) in water to form a solution; (B) primary drying at -10 - -40 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours to form lyophilized product; (C) secondary drying the resultant lyophilized product at 10 - 30 EC under high vacuum of 50 - 300 millitorr for 24 - 96 hours; and (D) packaging the lyophilized product in a first vial in combination with a second vial containing an equal mixture by volume of a nonionic surfactant and anhydrous ethanol. [Image] Q : M-CH(R 7&gt;)(CH 3) or CH=C(R 7&gt;); M : O, S, NR 8&gt; or CR 9&gt;R 1&gt; 0&gt;; R 1&gt; - R 5&gt;, R 7&gt; and R 1&gt; 1&gt; - R 1&gt; 5&gt;alkyl, aryl (both optionally substituted), H or heterocyclo; R 1&gt;+R 2&gt;cycloalkyl; R 6&gt;alkyl, aryl, heterocyclo (all optionally substituted) or H; R 8&gt;H, alkyl (optionally substituted), R 1&gt; 1&gt;C=O, R 1&gt; 2&gt;OC=O or R 1&gt; 3&gt;SO 2; and R 9&gt; and R 1&gt; 0&gt;H, halo, alkyl (optionally substituted), aryl, heterocyclo, hydroxy, R 1&gt; 4&gt;C=O or R 1&gt; 5&gt;OC=O. Independent claims are also included for: (1) A pharmaceutical preparation (II) comprising, in separate vials, lyophilized (I) and its solvent such that when the contents of the vials are combined, the resulting solution contains (I) (2 - 4 mg/ml). The solvent mixture comprises a mixture of about equal parts by volume of dehydrated ethanol and the nonionic surfactant; (2) Process for forming a pharmaceutical composition for parenteral administration; (3) Treating a patient involving administering to the patient by intravenous injection the (II); (4) Treating cancer involving intravenously and orally administering (I); (5) A pharmaceutical composition (III) for parenteral administration comprising (I), dehydrated alcohol and non-ionic surfactant; (6) Method of treating cancer in a patient previously experiencing neurotoxicity involving intravenously administering the composition diluted in a parenteral diluent as a weekly infusion in dose of less than 200 mg/m 2&gt;; (7) Treating cancer in a patient involving intravenously administering to the patient the formulation in a parenteral diluent; (8) Treating cancer by reducing or avoiding neurotoxicity involving intravenously infusing (I) over a period of one hour to the patient; and (9) Method of treating cancer in human patient with a synthetic or semi-synthetic epothilone analog involving a four week dosing cycle where the cycle comprises 3 weeks of weekly intravenous administration and one week of oral administration of the analog. ACTIVITY : Cytostatic; Antitumor; Anti-HIV; Antiarthritic; Antiinflammatory; Vasotropic; Neuroprotective; Osteopathic; Virucide; Dermatological; Immunosuppressive; Antirheumatic; Nootropic; Antiparkinsonian; Antiallergic; Antidiabetic; Antipsoriatic; Antidepressant; Antianemic; Cerebroprotective; Antiarrhythmic; Antiarteriosclerotic; Cardiant. No biological data available. MECHANISM OF ACTION : Apoptosis modulator. No biological data available.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title METHODS OF ADMINISTERING EPOTHILONE ANALOGS FOR THE TREATMENT OF CANCER
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