To assess the safety and effectiveness of SCH 39304 as primary treatment of acute cryptococcal meningitis in HIV-infected patients. Safety and effectiveness of maintenance therapy following successful treatment of acute disease are also evaluated.
Cryptococcal meningitis is a significant cause of illness and death in HIV-infected patients. Intravenous amphotericin B is effective for acute disease but relapse occurs in the majority of patients. Maintenance therapy is recommended but must be balanced against the multiple toxicities of the drugs used and the problems associated with the weekly administration of intravenous therapy. Treatments that are equally or more effective and less toxic than traditional methods are needed, especially oral therapy. SCH 39304 is an orally active antifungal drug that in animal studies is active against a wide range of systemic fungal infections including infections due to Cryptococcus. Features of SCH 39304 suggest that it might be of value in the treatment of cryptococcal meningitis.

Start Date-

Sponsor / Collaborator

National Institute of Allergy & Infectious Diseases

[+1]

100 Clinical Results associated with Genaconazole

100 Translational Medicine associated with Genaconazole

100 Patents (Medical) associated with Genaconazole

Literatures (Medical) associated with Genaconazole

01 Sep 2023·Journal of Biochemical and Molecular Toxicology

An extensive review on antifungal approaches in the treatment of mucormycosis

Review

Author: Palkar, Omkar S ; Abha Mishra, K M ; Chaudhari, Hrushikesh S ; Sethi, Kalyan K

AbstractDuring the period of COVID‐19, the occurrences of mucormycosis in immunocompromised patients have increased significantly. Mucormycosis (black fungus) is a rare and rapidly progressing fungal infection associated with high mortality and morbidity in India as well as globally. The causative agents for this infection are collectively called mucoromycetes which are the members of the orderMucorales. The diagnosis of the infection needs to be performed as soon as the occurrence of clinical symptoms which differs with types ofMucoralesinfection. Imaging techniques magnetic resonance imaging or computed tomography scan, culture testing, and microscopy are the approaches for the diagnosis. After the diagnosis of the infection is confirmed, rapid action is needed for the treatment in the form of antifungal therapy or surgery depending upon the severity of the infection. Delaying in treatment declines the chances of survival. In antifungal therapy, there are two approaches first‐line therapy (monotherapy) and combination therapy. Amphotericin B (1) and isavuconazole (2) are the drugs of choice for first‐line therapy in the treatment of mucormycosis. Salvage therapy with posaconazole (3) and deferasirox (4) is another approach for patients who are not responsible for any other therapy. Adjunctive therapy is also used in the treatment of mucormycosis along with first‐line therapy, which involves hyperbaric oxygen and cytokine therapy. There are some drugs like VT‐1161 (5) and APX001A (6), Colistin, SCH 42427, and PC1244 that are under clinical trials. Despite all these approaches, none can be 100% successful in giving results. Therefore, new medications with favorable or little side effects are required for the treatment of mucormycosis.

28 Jun 2008·Clinical and Experimental ImmunologyQ3 · MEDICINE

Effect of anti-IL-4, interferon-gamma and an antifungal triazole (SCH 42427) in paracoccidioidomycosis: correlation of IgE levels with outcome

Q3 · MEDICINE

Article

Author: STEVENS, D A ; COFFMAN, R L ; HOSTETLER, J S ; BRUMMER, E

SUMMARYParacoccidioidomycosis is characterized by depressed cellular but enhanced humoral immune responses, which suggests a Th2 type of response to infection. We investigated possible therapeutic roles for anti-IL-4, interferon-gamma (IFN-γ) and/or SCH 42427 (SCH), a new triazole antifungal agent, and their effect on serum IgE levels in a murine model of chronic Paracoccidioides brasiliensis infection. BALB/c mice infected by the pulmonary route were studied with three programmes. The subacute model and one acute model experiment investigated cytokine secretion by lymph node cells (LNC), and in a second acute experiment mice were given anti-IL-4, IFN-γ or nothing 24 h post infection, then killed at 4 weeks. In the chronic model, mice began treatment at 4 weeks post infection, receiving either SCH, IFN-γ alone, SCH + IFN-γ. or no treatment for 8 weeks. At 2-week intervals lung and spleen burdens of infection and serum polyclonal IgE levels were determined. In the subacute model (non-progressive infection), initially there was dual production of IL-4 and IFN-γ by antigen-stimulated LNC. In the acute progressive infection model IL-4, but not IFN-γ. was secreted. Anti-IL-4 treatment of the acute phase resulted in enhanced host resistance to infection, which correlated with decreased scrum IgE. The chronic model, in which the in vivo efficacy of SCH against P. brasiliensis was shown, suggests possible synergy between immunomodulation and antimicrobial chemotherapy (IFN-γ and SCH). Decreased organ burdens of infection in the chronic model after treatment with SCH, SCH plus IFN-γ, or anti-IL-4 correlated with decreased serum IgE. These promising novel approaches lo treatment of systemic fungal infections suggest a Th2 type of response to P. brasiliensis infection, which can be reversed with successful therapy.

01 Jan 2002·ChiralityQ4 · CHEMISTRY

Pharmacokinetics of the active antifungal enantiomer, SCH 42427 (RR), and evaluation of its chiral inversion in animals following its oral administration and the oral administration of its racemate genaconazole (RR/SS)

Q4 · CHEMISTRY

Article

Author: Amin A. Nomeir ; Raymond Lovey ; Elaine Radwanski ; Hong Kim ; Chin-Chung Lin

AbstractGenaconazole (SCH 39304) is a potent triazole antifungal agent that is active both orally and topically. Genaconazole is a racemic mixture which contains 50% of the RR (SCH 42427) and 50% of the SS (SCH 42426) enantiomers. The RR isomer accounts for most of the antifungal activity of genaconazole. Serum concentrations of the RR and SS enantiomers were analyzed by a chiral HPLC method which involved extraction of serum with organic solvent followed by separation on a Cyclobond I column and quantification by UV absorbance at 205 nm. The bioavailability and pharmacokinetic profiles of the two enantiomers after oral administration of the racemate (genaconazole) were very similar in cynomolgus monkeys. In rats following dosing with genaconazole, the RR enantiomer had a lower Cmax and a longer t1/2 than the SS enantiomer, while the AUC(I) values of the two enantiomers were similar. Based on chiral HPLC analysis, there was no evidence for the inversion of the RR to the SR isomer, or of the SS to the SR isomer, indicating that there was no chiral inversion of the RR or SS enantiomers in either species. Genaconazole at 20 mg/kg and the RR (SCH 42427) enantiomer at 10 mg/kg had very similar serum concentration–time profiles and Cmax, AUC(I), and t1/2 values for the RR enantiomer in both rats and monkeys, indicating that the two treatments were equivalent with respect to the bioavailability of the RR enantiomer. Chirality 14:436–441, 2002. © 2002 Wiley‐Liss, Inc.

100 Deals associated with Genaconazole

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Phase 3	US	Schering-Plough Corp.	31 Aug 2001
Meningitis, Cryptococcal	Phase 3	US	Schering-Plough Corp.	31 Aug 2001
Mycoses	Phase 3	-	Sumitomo Pharma Co., Ltd.	-
Mycoses	Phase 3	-	Merck Sharp & Dohme Corp.	-

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