EP1150670A2 - Agents d'alkylation destines au traitement de proliferation cellulaire - Google Patents
Agents d'alkylation destines au traitement de proliferation cellulaireInfo
- Publication number
- EP1150670A2 EP1150670A2 EP00914574A EP00914574A EP1150670A2 EP 1150670 A2 EP1150670 A2 EP 1150670A2 EP 00914574 A EP00914574 A EP 00914574A EP 00914574 A EP00914574 A EP 00914574A EP 1150670 A2 EP1150670 A2 EP 1150670A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- stent
- alkylating agent
- composition according
- agent
- polymer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Definitions
- the ethyleneimines and methylmelamines include the compounds triethylenemelamine, thiotepa (triethylene thiophosphoramide) and altretamine (hexamethylmelamine).
- Thiotepa and its primary metabolite, triethylenephosphoramide are capable of fo ⁇ ning DNA cross-links, as the aziridine rings open after protonation of the ring-nitrogen, leading to a reactive molecule.
- the alkyl sulfonates include busulfan.
- the nitrosoureas include carmustine and lomustine, semustine and streptozocin.
- the triazenes include dacarbazine.
- the alkylating agent melphalan was incorporated into polymer stents and implanted into pig coronary arteries, and this study will now be discussed.
- stents as depicted in Fig. 3C were prepared and loaded with melphalan and then placed in the coronary arteries of pigs. Preparation of the melphalan-loaded stents is described in Example 3.
- the stents, which carried a total drug load of 546 ⁇ g, were deployed into the pig coronary artery using a balloon catheter and positioned distally in the right coronary artery and approximately in the middle of the left circumflex artery.
- a commercially available metal stent not carrying a polymer member was also deployed into the left anterior descending artery.
- Stents carrying four polymer sleeve segments were prepared as described in Example 2.
- a solution of melphalan in methanol was prepared by dissolving 0.0293 g melphalan in 1.5 mL methanol to give a solution concentration of 19.5 ⁇ g/ ⁇ L.
- Each of the four segments was loaded with 136.5 ⁇ g of melphalan from the stock solution by pipetting 1 ⁇ L of the solution on each segment 7 times.
- the total drug loading in the polymer stent was 546 ⁇ g.
- the pig was euthanized and the heart and coronary arteries explanted.
- the arteries were pressure fixed for mo ⁇ hometric analysis to determine the percent diameter stenosis and percent intimal growth.
- the percent diameter stenosis was taken as l-[(stented vessel's minimum lumenal diameter)/(diameter of unstented reference vessel)]*100.
- the percent intimal growth was taken as l-[(stented vessel's minimum lumenal diameter)/(diameter of stented portion prior to stent placement)]* 100.
- the balloon to artery ratio was also determined as a measure of the degree of distension of the vessel by the balloon. The results are shown in Table 1.
- a solution of busulfan in dimethylsulfoxide was prepared by dissolving 0.0243 g busulfan in 300 ⁇ L dimethylsulfoxide to give a solution concentration of 81 ⁇ g/ ⁇ L.
- Each of the four segments was loaded with 81 ⁇ g of busulfan from the stock solution by pipetting 1 ⁇ L of the solution on each segment.
- the total drug loading in the polymer stent was 162 ⁇ g-
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)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US11995199P | 1999-02-12 | 1999-02-12 | |
US119951P | 1999-02-12 | ||
PCT/US2000/003667 WO2000047197A2 (fr) | 1999-02-12 | 2000-02-10 | Agents d'alkylation destines au traitement de proliferation cellulaire |
Publications (1)
Publication Number | Publication Date |
---|---|
EP1150670A2 true EP1150670A2 (fr) | 2001-11-07 |
Family
ID=22387376
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP00914574A Withdrawn EP1150670A2 (fr) | 1999-02-12 | 2000-02-10 | Agents d'alkylation destines au traitement de proliferation cellulaire |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP1150670A2 (fr) |
JP (1) | JP2002536406A (fr) |
AU (1) | AU3594700A (fr) |
CA (1) | CA2362883A1 (fr) |
WO (1) | WO2000047197A2 (fr) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2002246542A1 (en) * | 2000-10-31 | 2002-07-30 | Chemgenex Therapeutics, Inc. | Antiproliferative colchicine compositions and uses thereof |
DE10115740A1 (de) | 2001-03-26 | 2002-10-02 | Ulrich Speck | Zubereitung für die Restenoseprophylaxe |
US6537195B2 (en) | 2001-05-07 | 2003-03-25 | Xoft, Microtube, Inc. | Combination x-ray radiation and drug delivery devices and methods for inhibiting hyperplasia |
US7041046B2 (en) | 2001-05-07 | 2006-05-09 | Xoft, Inc. | Combination ionizing radiation and immunomodulator delivery devices and methods for inhibiting hyperplasia |
DE10244847A1 (de) | 2002-09-20 | 2004-04-01 | Ulrich Prof. Dr. Speck | Medizinische Vorrichtung zur Arzneimittelabgabe |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0518940A4 (en) * | 1990-02-26 | 1993-05-12 | Marvin J. Slepian | Method and apparatus for treatment of tubular organs |
US6057367A (en) * | 1996-08-30 | 2000-05-02 | Duke University | Manipulating nitrosative stress to kill pathologic microbes, pathologic helminths and pathologically proliferating cells or to upregulate nitrosative stress defenses |
CA2302438A1 (fr) * | 1997-05-19 | 1998-11-26 | Sugen, Inc. | Composes d'heteroarylcarboxamide actifs contre les etats pathologiques lies aux proteine tyrosine kinases |
DE69839077T2 (de) * | 1997-06-18 | 2009-01-22 | Boston Scientific Ltd., St. Michael | Polycarbonat-polyurethan-dispersion als gerinnungsbeständige beschichtung |
JP2002511878A (ja) * | 1997-07-01 | 2002-04-16 | アセロジエニクス・インコーポレイテツド | 抗酸化剤による過増殖状態の治療の増強 |
US6153252A (en) * | 1998-06-30 | 2000-11-28 | Ethicon, Inc. | Process for coating stents |
-
2000
- 2000-02-10 AU AU35947/00A patent/AU3594700A/en not_active Abandoned
- 2000-02-10 JP JP2000598150A patent/JP2002536406A/ja active Pending
- 2000-02-10 EP EP00914574A patent/EP1150670A2/fr not_active Withdrawn
- 2000-02-10 WO PCT/US2000/003667 patent/WO2000047197A2/fr not_active Application Discontinuation
- 2000-02-10 CA CA002362883A patent/CA2362883A1/fr not_active Abandoned
Non-Patent Citations (1)
Title |
---|
See references of WO0047197A2 * |
Also Published As
Publication number | Publication date |
---|---|
WO2000047197A2 (fr) | 2000-08-17 |
AU3594700A (en) | 2000-08-29 |
CA2362883A1 (fr) | 2000-08-17 |
WO2000047197A3 (fr) | 2001-04-05 |
JP2002536406A (ja) | 2002-10-29 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
|
17P | Request for examination filed |
Effective date: 20010821 |
|
AK | Designated contracting states |
Kind code of ref document: A2 Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE |
|
AX | Request for extension of the european patent |
Free format text: AL;LT;LV;MK;RO;SI |
|
RIN1 | Information on inventor provided before grant (corrected) |
Inventor name: POMERANTSEVA, IRINA, D. Inventor name: ALVARADO, ANGELICA Inventor name: EURY, ROBERT Inventor name: FROIX, MICHAEL |
|
17Q | First examination report despatched |
Effective date: 20030925 |
|
RBV | Designated contracting states (corrected) |
Designated state(s): DE FR GB IE NL |
|
STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
|
18D | Application deemed to be withdrawn |
Effective date: 20040206 |