Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/16—Amides, e.g. hydroxamic acids
  • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P35/00—Antineoplastic agents

Definitions

• Antitumor combination combining AVE8062 and docetaxel
• the present invention relates to an antitumor combination combining 1 ⁇ VE8062 or a salt of 1 ⁇ VE8062 and docetaxel in the treatment of solid tumors.
• WO 02/056692 discloses combinations of a combretastatin A-4 and two anti-cancer agents. Among the examples given, combretastatin A-4 at a dose of 1-100 mg / m is combined with paclitaxel at a dose of 40-250 mg / m 2 .
• WO 2006/078422 also discloses a combination of a combretastatin at a dose of 1-100 mg / m and paclitaxel at a dose of 40-250 mg / m 2 .
• WO 02/074229 describes the combination of 1 ⁇ VE8062 and an anticancer agent chosen from taxanes, especially taxol or docetaxel, vinca alkaloids, alkylating agents, antimetabolites.
• the combination may be to administer both compounds at the same time or sequentially. The order of administration is not specified.
• the compounds can be administered orally, intravenously, subcutaneously or intramuscularly.
• a taxane In the case of a taxane, it is administered by intraperitoneal injection at a dose of between 1 and 10 mg / kg or intravenously at a dose of between 1 and 3 mg / kg. Examples are given in mice of 1 ⁇ VE8062 at a dose of 150 mg / kg and docetaxel at a dose of 109.6 mg / kg (AVE8062A / docetaxel ratio: 1.37).
• mice of 1 ⁇ VE8062 at a dose of 150 mg / kg
• docetaxel at a dose of 109.6 mg / kg (AVE8062A / docetaxel ratio: 1.37).
• AVE8062A / docetaxel ratio 1.37
• mice By taking a mouse-to-mouse conversion factor of 3 in the mouse case (see Freireich, EJ "Quantitative comparison of toxicity of anticancer agents in mouse, rat, dog, monkey and man.” Cancer Chemother Rep. 1966, 50 (4) , 219-244), this results
• LVE8062A was administered in the mouse at a dose of 10, 30, 50 and 100 mg / kg (30-300 mg / m 2 ) and docetaxel at a dose of 2 or 1.4 mg / kg (6 or 4, 2 mg / m). The dose of 30 mg / kg is that recommended for 1 ⁇ VE8062.
• NCT00719524 of a combination AVE8062 + cis-platinum (D1) / docetaxel (D2) in the treatment of patients with advanced solid tumor is presented. No dose is specified.
• the invention relates to an antitumor and sequential combination of AVE8062 or a salt of AVE8062 and docetaxel characterized in that 1 ⁇ VE8062 is administered to a patient at a dose of between 10 and 50 mg / m 2 and then a day different from the week, preferably after a 24 hour interval, docetaxel at a dose of between 50 and 120 mg / m 2 .
• the dose of AVE8062 or the salt of AVE8062 is rather 20-40 mg / m 2 , rather 30-40 mg / m.
• the dose of docetaxel is rather 50-100 mg / m, rather 60-80 mg / m 2 .
• the dose of AVE8062 or the salt of AVE8062 may be 35 mg / m 2 and that of docetaxel 75 mg / m 2 .
• LVE8062 or AVE8062 salt and docetaxel can be administered by infusion.
• the invention also relates to a combination for administration to a patient during a cycle comprising administration of AVE8062 or AVE8062 salt marking the beginning of the cycle followed by administration of docetaxel characterized in that 1 ⁇ VE8062 or the salt of AVE8062 is administered first and then a different day of the week, preferably after a period of 24 hours, is administered docetaxel, the doses of AVE8062 and docetaxel being as defined in one of the Claims 1 to 4.
• the cycle may be repeated, the interval between two administrations of AVE8062 or AVE8062 salt is from 1 to 4 weeks, preferably 3.
• the invention also relates to the use of 1 ⁇ VE8062 or a salt of AVE8062 and docetaxel for the preparation of an antitumor combination as defined in one of claims 1 to 10.
• the invention also relates to the use of 1 ⁇ VE8062 or a salt of AVE8062 for the preparation of an antitumor combination as defined in one of claims 1 to 10.
• the combination makes it possible to treat a solid tumor. It can treat breast cancer, ovarian, esophagus, pancreas, muscle tissue or soft tissue, cancer head / neck, bladder, liver, prostate, prostate ovary or skin.
• AVE8062A designates the hydrochloride of 1 ⁇ VE8062.
• the EV8062 can be prepared according to the method described in WO 03/084919.
• 1 ⁇ VE8062A was used; this compound is packaged in the form of a vial containing an aqueous solution of the active ingredient. Approximately 25 mg of AVE8062A is withdrawn from the vial and diluted in an infusion bag prior to administration to the patient. The concentration of AVE8062A in the pouch is between 0.012 mg / ml and 1.62 mg / ml. The infusion volume administered to each patient depends on the patient.
• docetaxel it is marketed under the brand name
• Taxotere * by Sanofi-Aventis It has the chemical formula:
• docetaxel It may be a form having as CAS No. 114977-28-5 or 148408-66-6 (trihydrate).
• the preparation of docetaxel is described for example in EP 0253738, EP 0253739 and WO 92/09589.
• docetaxel was packaged in a vial containing anhydrous docetaxel in polysorbate 80 at a concentration of 40 mg / ml.
• a vial containing 20 mg docetaxel (0.5 ml) can be used, which is then diluted with the contents of one vial (1.98 ml) of 13% w / w aqueous ethanol solution. to obtain a premix solution having a final concentration of docetaxel at 10 mg / ml.
• a vial containing 80 mg of docetaxel (2 ml) can also be used, which is then diluted with the contents of one vial (7.33 ml) of a 13% w / w aqueous solution of ethanol. to obtain a premix solution having a final concentration of docetaxel at 10 mg / ml.
• the premix solution is then rediluted in an infusion bag containing glucose or sodium chloride.
• the infusion volume administered to each patient depends on the patient.
• this consists in sequentially administering, preferably by infusion, 1 ⁇ VE8062 or a salt of 1 ⁇ VE8062, at a dose of between 10 and 50 mg / m 2 , and then on a different day of the week. preferably after an interval of 24 hours, docetaxel at a dose of between 50 and 120 mg / m. It is preferable to combine the two compounds sequentially and in this order, ie first 1 ⁇ VE8062 or the salt of 1 ⁇ VE8062, then docetaxel.
• the dose of AVE8062 or the salt of 1 ⁇ VE8062 is 20-40 mg / m 2 , rather 30-40 mg / m 2 and / or the dose of docetaxel is 50-100 mg / m 2 , rather 60-80 mg / m 2 .
• a combination may be for example 35 mg / m 2 of AVE8062 or the salt of 1 ⁇ VE8062 and 75 mg / m 2 of docetaxel.
• the protocol consisted of administering a combination of AVE8062A and docetaxel to patients with advanced solid tumors. I / AVE8062A is administered by infusion over a period of about 30 minutes and the next day, docetaxel is administered by infusion over a period of about one hour. This cycle AVE8062A / docetaxel is then repeated every three weeks.
• the tumor it may be a solid tumor, particularly that of the adult or the child.
• the combination can treat breast cancer, ovarian cancer, esophagus, pancreas, muscle tissue or soft tissue, cancer head / neck, bladder, liver, prostate, prostate ovary or skin.

Landscapes

• Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Epidemiology (AREA)
• Pain & Pain Management (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Oncology (AREA)
• Communicable Diseases (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines Containing Material From Animals Or Micro-Organisms (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=40790630

Family Applications (1)

Country Status (27)

Family Cites Families (7)

• 2008
  • 2008-12-12 FR FR0806979A patent/FR2939665B1/fr not_active Expired - Fee Related
• 2009
  • 2009-12-10 CN CN2009801497729A patent/CN102245175A/zh active Pending
  • 2009-12-10 MA MA34002A patent/MA32955B1/fr unknown
  • 2009-12-10 PE PE2011001197A patent/PE20120125A1/es not_active Application Discontinuation
  • 2009-12-10 SG SG2011042348A patent/SG172071A1/en unknown
  • 2009-12-10 AU AU2009326220A patent/AU2009326220A1/en not_active Abandoned
  • 2009-12-10 EA EA201170803A patent/EA201170803A1/ru unknown
  • 2009-12-10 WO PCT/FR2009/052475 patent/WO2010067027A1/fr active Application Filing
  • 2009-12-10 CA CA2746475A patent/CA2746475A1/fr not_active Abandoned
  • 2009-12-10 MX MX2011006253A patent/MX2011006253A/es not_active Application Discontinuation
  • 2009-12-10 KR KR1020117013250A patent/KR20110104932A/ko not_active Application Discontinuation
  • 2009-12-10 EP EP09802160A patent/EP2376076A1/fr not_active Withdrawn
  • 2009-12-10 JP JP2011540175A patent/JP2012511554A/ja active Pending
  • 2009-12-10 TW TW098142340A patent/TW201032798A/zh unknown
  • 2009-12-10 BR BRPI0923349-0A patent/BRPI0923349A2/pt not_active IP Right Cessation
  • 2009-12-11 AR ARP090104814A patent/AR074599A1/es not_active Application Discontinuation
  • 2009-12-11 PA PA20098853301A patent/PA8853301A1/es unknown
  • 2009-12-11 UY UY0001032318A patent/UY32318A/es not_active Application Discontinuation
• 2011
  • 2011-05-24 TN TN2011000268A patent/TN2011000268A1/fr unknown
  • 2011-06-02 CL CL2011001316A patent/CL2011001316A1/es unknown
  • 2011-06-06 US US13/153,975 patent/US20120004294A1/en not_active Abandoned
  • 2011-06-07 EC EC2011011112A patent/ECSP11011112A/es unknown
  • 2011-06-08 CR CR20110319A patent/CR20110319A/es unknown
  • 2011-06-08 NI NI201100114A patent/NI201100114A/es unknown
  • 2011-06-09 IL IL213458A patent/IL213458A0/en unknown
  • 2011-06-10 ZA ZA2011/04358A patent/ZA201104358B/en unknown
  • 2011-06-10 CO CO11072133A patent/CO6390037A2/es not_active Application Discontinuation

Non-Patent Citations (1)

Also Published As

Similar Documents

Legal Events