USRE38984E1 - Antifungal combination therapy - Google Patents
Antifungal combination therapy Download PDFInfo
- Publication number
- USRE38984E1 USRE38984E1 US10/325,137 US32513799D USRE38984E US RE38984 E1 USRE38984 E1 US RE38984E1 US 32513799 D US32513799 D US 32513799D US RE38984 E USRE38984 E US RE38984E
- Authority
- US
- United States
- Prior art keywords
- spp
- inhibitor
- cryptococcus
- azole
- compound
- 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.)
- Expired - Lifetime
Links
- JYIKNQVWKBUSNH-OGZDCFRISA-N [H][C@@]1([C@H](O)[C@@H](O)C2=CC=C(O)C=C2)NC(=O)[C@]2([H])C[C@@H](O)CN2C(=O)[C@]([H])([C@@H](C)O)NC(=O)[C@@H](NC(=O)CCCCCCCCC(C)CC(C)CC)C[C@@H](O)[C@@H](NCCN)NC(=O)[C@]2([H])[C@@H](O)CCN2C(=O)[C@]([H])([C@H](O)CCN)NC1=O Chemical compound [H][C@@]1([C@H](O)[C@@H](O)C2=CC=C(O)C=C2)NC(=O)[C@]2([H])C[C@@H](O)CN2C(=O)[C@]([H])([C@@H](C)O)NC(=O)[C@@H](NC(=O)CCCCCCCCC(C)CC(C)CC)C[C@@H](O)[C@@H](NCCN)NC(=O)[C@]2([H])[C@@H](O)CCN2C(=O)[C@]([H])([C@H](O)CCN)NC1=O JYIKNQVWKBUSNH-OGZDCFRISA-N 0.000 description 5
- JYIKNQVWKBUSNH-QWDBRQCVSA-N CCC(C)CC(C)CCCCCCCCC(NC(C[C@H]([C@@H](NCCN)NC([C@H]([C@H](CC1)O)N1C([C@H]([C@@H](CCN)O)NC([C@H]([C@@H]([C@H](c(cc1)ccc1O)O)O)NC([C@H](C[C@H](C1)O)N1C([C@H]([C@@H](C)O)N1)=O)=O)=O)=O)=O)O)C1=O)=O Chemical compound CCC(C)CC(C)CCCCCCCCC(NC(C[C@H]([C@@H](NCCN)NC([C@H]([C@H](CC1)O)N1C([C@H]([C@@H](CCN)O)NC([C@H]([C@@H]([C@H](c(cc1)ccc1O)O)O)NC([C@H](C[C@H](C1)O)N1C([C@H]([C@@H](C)O)N1)=O)=O)=O)=O)=O)O)C1=O)=O JYIKNQVWKBUSNH-QWDBRQCVSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- A61K38/1751—Bactericidal/permeability-increasing protein [BPI]
Definitions
- the present invention relates to antifungal combination therapy comprising the use of known antifungal agents such as the azoles or polyenes in combination with a pneumocandin derivative antifungal agent. More particularly, the invention relates to antifungal combination therapy comprising the use of azoles such as fluconazole (hereinafter referred to as FCZ), voriconazole, itraconazole, ketoconazole, miconazole, ER 30346, SCH 56592; polyenes such as amphotericin B (hereinafter referred to as AmB), nystatin or liposomal and lipid forms thereof such as Abelcet, AmBisome and Amphocil; purine or pyrimidine nucleotide inhibitors such as flucytosine; or polyoxins such as nikkomycins, in particular nikkomycin Z or other chitin inhibitors, elongation factor inhibitors such as sordarin and analogs thereof, mannan inhibitors such as preda
- the present treatments i.e., polyenes, such as amphotericin B, cause severe side effects and azoles, such as fluconazole, are only fungistatic.
- the pneumocandins which are related to the echinocandins, are cyclic hexapeptides which inhibit cell wall 1,3 ⁇ -D-glucan synthesis.
- the pneumocandins have shown potent in vivo activity against Candida spp., Pneumocystis carinii, Aspergillus spp., as well as the other fungal pathogens listed above.
- the pneumocandins by themselves, have weak activity against Cryptococcus spp.
- Combination therapy with antifungal drugs may provide additional options for treating Cryptococcus and other fungal pathogens.
- the present invention relates to antifungal combination therapy comprising the use of known antifungal agents such as the azoles or polyenes in combination with a pneumocandin derivative antifungal agent. More particularly, the invention relates to antifungal combination therapy comprising the use of azoles such as fluconazole, voriconazole, itraconazole, ketoconazole, miconazole, ER 30346, SCH 56592; polyenes such as amphotericin B, nystatin or liposomal and lipid forms thereof such as Abelcet, AmBisome and Amphocil; purine or pyrimidine nucleotide inhibitors such as flucytosine; or polyoxins such as nikkomycins, in particular nikkomycin Z or other chitin inhibitors, elongation factor inhibitors such as sordarin and analogs thereof, mannan inhibitors such as predamycin , bactericidal/permeability-inducing (BPI) protein
- this combination therapy has been shown to be useful against such opportunistic pathogens as Cryptococcus spp., Candida spp., Aspergillus spp., Histoplasma spp., Coccidioides spp., Paracoccidioides spp.
- pneumocandin derivatives such as those disclosed in U.S. Pat. No. 5,516,756 and in copending applications 07/936,558, 07/936,561, 09/058,657, 09/055,996, 08/378,687 and 60/006,505 would be useful in the combination therapy.
- the azole, polyene or other antifungal agent may be administered orally or parenterally.
- Compound I is preferably administered parenterally, but is not limited to that route and may also be administered by other routes such as oral, intramuscular or subcutaneous.
- the combination therapy results in enhanced effects using sub-inhibitory concentrations of all agents. These effects can be demonstrated in vitro and in vivo using clinical and environmental strains of C. neoformans, C. albicans and A. fumigatus.
- the minimal inhibitory concentrations (MICS) for AmB and Compound I were defined as the lowest drug concentration at which there was an absence of growth.
- FCZ MIC was defined as the lowest drug concentration which resulted in a visual turbidity less than or equal to 80% inhibition compared with that produced by the control without antifungal agent.
- CFUs colony forming units
Abstract
Description
or a pharmaceutically acceptable salt or other pharmaceutically acceptable formulation thereof.
or a pharmaceutically acceptable salt or other pharmaceutically acceptable formulation thereof.
Claims (15)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10/325,137 USRE38984E1 (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US2632796P | 1996-09-12 | 1996-09-12 | |
US09/242,831 US6069126A (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
US10/325,137 USRE38984E1 (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
PCT/US1997/015987 WO1998010782A1 (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
Publications (1)
Publication Number | Publication Date |
---|---|
USRE38984E1 true USRE38984E1 (en) | 2006-02-14 |
Family
ID=26701092
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US09/242,831 Ceased US6069126A (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
US10/325,137 Expired - Lifetime USRE38984E1 (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US09/242,831 Ceased US6069126A (en) | 1996-09-12 | 1997-09-09 | Antifungal combination therapy |
Country Status (1)
Country | Link |
---|---|
US (2) | US6069126A (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060293381A1 (en) * | 2005-06-23 | 2006-12-28 | Kaihei Kojima | Fungicidal effect by regulating signal transduction pathways |
US9636407B2 (en) | 2012-11-20 | 2017-05-02 | Fresenius Kabi Usa, Llc | Caspofungin acetate formulations |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060172007A1 (en) * | 2001-05-01 | 2006-08-03 | Nawaz Ahmad | Compositions and methods for reducing vaginal pH |
US20030017207A1 (en) * | 2001-05-01 | 2003-01-23 | Lin Shun Y. | Compositions and methods for treating vulvovaginitis and vaginosis |
US20030064103A1 (en) * | 2001-05-01 | 2003-04-03 | Lin Shun Y. | Compositions and methods for treating vulvovaginitis and vaginosis |
WO2003051889A1 (en) * | 2001-12-14 | 2003-06-26 | Merck & Co., Inc. | A novel sordarin derivative isolated from culture fermentations and functions as an antifungal agent |
US20060105008A1 (en) * | 2002-03-28 | 2006-05-18 | Nawaz Ahmad | Compositions and methods for reducing vaginal pH |
US7763660B2 (en) * | 2003-02-05 | 2010-07-27 | The University Of Vermont And State Agricultural College | Inhibitors of Candida albicans |
US20060194769A1 (en) * | 2005-01-25 | 2006-08-31 | University Of Vermont And State Agricultural College | Small molecules that reduce fungal growth |
LT3677252T (en) | 2012-03-19 | 2023-10-10 | Cidara Therapeutics, Inc. | Dosing regimens for echinocandin class compounds |
EP3399995A4 (en) * | 2016-01-08 | 2019-08-21 | Cidara Therapeutics, Inc. | Methods for preventing and treating pneumocystis infections |
EP4268896A3 (en) | 2016-03-16 | 2024-01-03 | Cidara Therapeutics, Inc. | Dosing regimens for treatment of fungal infections |
CA3069423A1 (en) | 2017-07-12 | 2019-01-17 | Cidara Therapeutics, Inc. | Formulations for the treatment of fungal infections |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5030619A (en) * | 1990-04-16 | 1991-07-09 | Miles Inc. | Synergistic fungicidal composition |
US5348970A (en) * | 1993-09-22 | 1994-09-20 | Merck & Co., Inc. | Antifungal compound and compositions containing the compound |
WO1994021677A1 (en) | 1993-03-16 | 1994-09-29 | Merck & Co., Inc. | Aza cyclohexapeptide compounds |
US5552521A (en) * | 1995-02-10 | 1996-09-03 | Merck & Co., Inc. | Process for preparing certain aza cyclohexapeptides |
US5627153A (en) * | 1994-01-14 | 1997-05-06 | Xoma Corporation | Anti-fungal methods and materials |
WO1998010782A1 (en) | 1996-09-12 | 1998-03-19 | Merck & Co., Inc. | Antifungal combination therapy |
US5741775A (en) * | 1993-05-04 | 1998-04-21 | Merck & Co., Inc. | Cyclohexapeptidyl aminoalkyl ethers |
-
1997
- 1997-09-09 US US09/242,831 patent/US6069126A/en not_active Ceased
- 1997-09-09 US US10/325,137 patent/USRE38984E1/en not_active Expired - Lifetime
Patent Citations (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5030619A (en) * | 1990-04-16 | 1991-07-09 | Miles Inc. | Synergistic fungicidal composition |
WO1994021677A1 (en) | 1993-03-16 | 1994-09-29 | Merck & Co., Inc. | Aza cyclohexapeptide compounds |
US5378804A (en) * | 1993-03-16 | 1995-01-03 | Merck & Co., Inc. | Aza cyclohexapeptide compounds |
HU211890A9 (en) | 1993-03-16 | 1995-12-28 | Merck & Co Inc | Aza cyclohexapeptide compounds |
US5514650A (en) * | 1993-03-16 | 1996-05-07 | Merck & Co., Inc. | Aza cyclohexapeptide compounds |
US5741775A (en) * | 1993-05-04 | 1998-04-21 | Merck & Co., Inc. | Cyclohexapeptidyl aminoalkyl ethers |
US5348970A (en) * | 1993-09-22 | 1994-09-20 | Merck & Co., Inc. | Antifungal compound and compositions containing the compound |
US5627153A (en) * | 1994-01-14 | 1997-05-06 | Xoma Corporation | Anti-fungal methods and materials |
US5552521A (en) * | 1995-02-10 | 1996-09-03 | Merck & Co., Inc. | Process for preparing certain aza cyclohexapeptides |
WO1998010782A1 (en) | 1996-09-12 | 1998-03-19 | Merck & Co., Inc. | Antifungal combination therapy |
Non-Patent Citations (14)
Title |
---|
Abruzzo, et al., Antimicrobial Agents & Chemotherapy (May 1995), pp. 1077-1081. |
Abstracts of the 36th ICAAC, Sep. 15-18, 1996, Tuesday, Session 83, p. 132. * |
Abstracts of the 36th ICAAC, Sep. 18-Oct. 1, 1997, pp. 162-163. |
Abstracts of the 37th ICAAC, Sep. 28-Oct. 1, 1997, pp. 162-163. * |
Antimicrobial Agents & Chemotherapy, pp. 1070-1076 (May 1995), by K. Barizal, et al. * |
Antimicrobial Agents & Chemotherapy, pp. 1077-1081 (May 1995), by G. Abruzzo, et al. * |
Antimicrobial Agents & Chemotherapy, vol. 41, No. 10, pp. 2310-2311 (1997), by D. Law, et al. * |
Antimicrobial Agents & Chemotherapy, vol. 41, No. 2, pp. 331-336 (1997), by S. Franzot, et al. * |
Antimicrobial Agents & Chemotherapy, vol. 42, No. 2, pp. 313-318 (1998), by J. Fung-Tomc, et al. * |
Franzot et al., Pneumocandin L-743,872 enhances the activities of amphotericin B and Fluconazole against Cryptococcus neoformans in vitro, Antimicrob. Agents Chemother., (1997), 41(2), 331-336 (abs.). * |
Franzot, et al. ICAAC Abstract No. 821, entitled "Pneumocandin L-743,872 enhances the activity of Amphotericin B and Fluconazole against Cryptococcus neoformans in vitro". |
Fung-Tomc, J., et al. Antimicrobial Agents & Chemotherapy, vol. 42, No. 2, pp. 313-318, 1998. |
ICAAC Abstract No. 821, entitled Pneumocandin L-7543-872 enhances the activity of Amphotericin B and Fluconazole against Cryprococcus neoformans in vitro by S. P. Franzot, et al. * |
Law, D., et al. Antimicrobial Agents & Chemotherapy, vol. 41, No. 10, pp. 2310-2311, 1997. |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060293381A1 (en) * | 2005-06-23 | 2006-12-28 | Kaihei Kojima | Fungicidal effect by regulating signal transduction pathways |
US9636407B2 (en) | 2012-11-20 | 2017-05-02 | Fresenius Kabi Usa, Llc | Caspofungin acetate formulations |
Also Published As
Publication number | Publication date |
---|---|
US6069126A (en) | 2000-05-30 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FPAY | Fee payment |
Year of fee payment: 8 |
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AS | Assignment |
Owner name: MERCK SHARP & DOHME CORP.,NEW JERSEY Free format text: CHANGE OF NAME;ASSIGNOR:MERCK & CO., INC.;REEL/FRAME:023870/0001 Effective date: 20091102 Owner name: MERCK SHARP & DOHME CORP., NEW JERSEY Free format text: CHANGE OF NAME;ASSIGNOR:MERCK & CO., INC.;REEL/FRAME:023870/0001 Effective date: 20091102 |
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FPAY | Fee payment |
Year of fee payment: 12 |
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AS | Assignment |
Owner name: SCHERING CORPORATION, NEW JERSEY Free format text: MERGER;ASSIGNOR:MERCK SHARP & DOHME CORP.;REEL/FRAME:028850/0515 Effective date: 20120426 |
|
AS | Assignment |
Owner name: MERCK SHARP & DOHME CORP., NEW JERSEY Free format text: CHANGE OF NAME;ASSIGNOR:SCHERING CORPORATION;REEL/FRAME:028866/0511 Effective date: 20120502 |