摘要:

&NA;Caspofungin (MK 991, L 743872, MK 0991), a pneumocandin derivative, is an injectable broad spectrum fungicidal agent that is in late phase II trials with Merck & Co in the US for the treatment of serious fungal infections. It is in preclinical trials in Brazil. Caspofungin also has potential in the treatment ofPneumocystis cariniipnuemonia in immunocompromised patients and is undergoing preclinical trials in this indication. It has limited oral activity, but may be useful in the oral treatment of oropharyngeal and gastrointestinal candidiasis.Caspofungin is the first glucan synthase inhibitor to be developed as an injectable antifungal for systemic candidiasis and aspergillosis. It appears to have similar efficacy to amphotericin B but is less toxic. Poor oral bioavailability will limit it to parenteral formulations.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;Eberconazole (WAS 2160) is a topical antifungal agent that is in phase III clinical trials with SALVAT and Wassermann-SEEFT in Spain. The compound is being compared with clotrimoxazole in 440 patients with dermatophysis, candidiasis or pityriasis versicolor. SALVAT has acquired exclusive worldwide rights to eberconazole from Wasserman and is looking for a development and marketing partner for European countries other than Spain.Eberconazole is active against most kinds of yeasts and dermatophytes and has very good local tolerability.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;ER 30346 (BMS 207147) is an orally active triazole antifungal agent with broad spectrum activity that is undergoing phase I investigation with Eisai in Japan and with Bristol-Myers Squibb in the USA. Bristol-Myers Squibb have licensed ER 30346 from Eisai for development worldwide, except for Japan where ER 30346 will continue to be developed by Eisai. ER 30346 has potential in the treatment of systemic fungal infections such as candidiasis, aspergillosis and cryptococcal meningitis and in the treatment of oropharyngeal candidiasis.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;FK 463 is a glucan synthase inhibitor that is being developed by Fujisawa as an antifungal agent. It is in phase II trials in Japan and the USA.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

IB 367 is a protegrin (a lytic peptide originally isolated from pig leucocytes) that is in phase II of development with IntraBiotics Pharmaceuticals in Europe and the US for the treatment and prevention of oral mucositis. Oral mucositis is a common adverse effect of cancer therapies, in which the rapidly growing epithelial cells that line the mouth are destroyed. IB 367 targets Gram negative and positive bacteria and Candida albicans, and destroys these pathogens by attaching to their lipid membranes; this sterilises the oral environment and prevents the likelihood of secondary infection if the atrophied mucosa is traumatised.Pharmacia & Upjohn will collaborate with IntraBiotics Pharmaceuticals for development and marketing of IB 367. Pharmacia & Upjohn has licensed worldwide exclusive rights to IB 367, except in the US. Under the licensing agreement, Pharmacia & Upjohn will receive up to $US35 million in licensing fees, milestone payments and equity investments.It appears that IntraBiotics has also signed an agreement with Polypeptide Laboratories A/S of Denmark for the development of a manufacturing process and for the supply of IB 367.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;LY 303366 (ECB) is an orally active antifungal agent that is in phase II clinical trials with Eli Lilly in the UK and US for the treatment ofCandida, AspergillusandPneumocystis cariniiinfections. An intravenous formulation of LY 303366 is undergoing preclinical investigation, but the poor water solubility of the compound may pose problems for this formulation. Follow-up compounds with improved water solubility, such as LY 333006 and LY 329960, are in preclinical development.LY 303366 is the lead compound from a series of lipopeptide echinocandin B derivatives that act by inhibiting the &bgr;1,3-glucan synthesis essential for fungal cell wall formation.LY 303366 is being developed for the treatment of candidiasis, aspergillosis and Pneumocystis carinii pneumonia. It is the first orally available glucan synthase inhibitor to reach clinical trials. Poor water solubility limits the IV formulation.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

Nikkomycin Z (SP 920704) is an orally active antifungal agent licensed to Shaman Pharmaceuticals from Bayer. It is currently undergoing phase I trials in the UK as monotherapy for coccidioidomycosis and preclinical testing in combination with azoles or echinocandins in the USA for the indication of endemic mycoses.Shaman Pharmaceuticals have filed an IND (Investigational New Drug) application in the US for the treatment of systemic fungal infections. Nikkomycin Z is a competitive chitin synthase inhibitor that has been evaluated in mouse models of coccidioidomycosis, histoplasmosis and blastomycosis. The limited toxicology tests conducted so far suggest that Nikkomycin Z is well tolerated at the dosages used.Nikkomycin Z is the first of a new class of antifungals (chitin synthesis inhibitors) to be developed but its poor potency means it will probably be used in combination with azoles or candins, except for coccidioidomycosis.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;Liposomal nystatin (AR 121, Nyotran®) is a lipid-based intravenous formulation of nystatin that is being developed by Aronex. Phase III trials comparing liposomal nystatin to standard amphotericin B treatment in immunocompromised cancer patients with suspected systemic fungal infections are underway in Europe and the US. A phase III study in patients with Cryptococcal meningitis is also underway, and a phase II trial in non-neutropenic patients with candidaemia has been completed in the US. Together with development partner Grupo Ferrer, Aronex has submitted a Marketing Authorisation Application in Portugal and Spain and expects to file for registration in other European countries in 1998. The company also plans to submit a US new drug application for this indication in 1999. Liposomal nystatin appears to have antiviral activity and is under phase II development for the treatment of HIV infection.Aronex Pharmaceuticals have signed a licensing agreement with Abbott Laboratories for worldwide rights to Nyotran®. Under this agreement, Abbott will provide funding for the clinical development of the drug, will market it after it is approved and will be responsible for its registration in countries outside the USA. Aronex will be able to copromote Nyotran® in Canada and the US for at least 2 years.Nystatin is a tetraene-diene polyene antibiotic complex that is widely established as an antifungal agent. It has been used as an oral and topical antifungal agent but was too toxic to use intravenously. This liposomal formulation is less toxic.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;SCH 56592 is an orally active triazole derivative that is in clinical trials with Schering-Plough in Canada and the US for the treatment of oral candidiasis. It is also undergoing preclinical investigation for the treatment of aspergillosis. In addition, SCH 56592 has potential in the treatment of Chagas disease, a condition caused by the protozoan parasiteTrypanosoma cruzi, and preclinical investigation is underway for this indication in Venezuela.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS

摘要:

&NA;Voriconazole (UK 109496) is a broad spectrum triazole antifungal agent that is in phase III trials with Pfizer in the UK and US for the treatment of resistant systemic candidiasis and invasive aspergillosis. It is also undergoing clinical investigation for oral candidiasis and oesophageal candidiasis.Pfizer hopes to market voriconazole in 2001/2002.Voriconazole is a new triazole antifungal which has a broader spectrum of action than fluconazole and is more potent. Unlike itraconazole, it can be administered either orally or parenterally. Although it may be more effective than currently available triazoles, it has the same problems with drug interactions and adverse events that affect itraconazole.

ISSN:1174-5886    

出版商:ADIS    

年代:1999

数据来源: ADIS