Delving into the Latest Updates on Fiacitabine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

FIAC, FOAC, Fiacitabine (USAN/INN)

+ [2]

Target

UL30 x UL54

Action

inhibitors

Mechanism

UL30 inhibitors(Human herpesvirus 1 DNA polymerase inhibitors), UL54 inhibitors(Human herpesvirus 5 DNA polymerase inhibitors)

Therapeutic Areas

Infectious DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Cytomegalovirus InfectionsHerpes Simplex

Originator Organization

Memorial Sloan Kettering Cancer Center

Active Organization-

Inactive Organization

Memorial Sloan Kettering Cancer CenterAllergan UCOclassen Pharmaceuticals

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC9H11FIN3O4

InChIKeyGIMSJJHKKXRFGV-BYPJNBLXSA-N

CAS Registry69123-90-6

To find oral doses of FIAC (a pyrimidine nucleoside analog) that are effective in treating cytomegalovirus (CMV) viremia in HIV-infected immunocompromised patients; to determine tolerance and safety of FIAC in this patient population; and to determine pharmacokinetics following multiple doses of FIAC. (An example of another nucleoside analog effective against retroviruses such as HIV is zidovudine (AZT).) CMV infection is a medically significant opportunistic disease in patients with HIV-related infection. The purine nucleoside ganciclovir has been used to treat AIDS patients with CMV disease. Although ganciclovir is useful in treating CMV disease, such treatment is frequently complicated by hematologic (blood) toxicity. Also, treatment is difficult because it requires daily intravenous dosing. Test tube studies show that FIAC and its primary breakdown product FIAU are highly and specifically active against several viruses including CMV. A single-dose, pharmacokinetic (blood level) study showed that FIAC, when taken orally, is readily absorbed into the bloodstream, and most of it is converted to FIAU.

Start Date-

Sponsor / Collaborator

National Institute of Allergy & Infectious Diseases

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100 Clinical Results associated with Fiacitabine

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100 Translational Medicine associated with Fiacitabine

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100 Patents (Medical) associated with Fiacitabine

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127

Literatures (Medical) associated with Fiacitabine

01 Dec 2024·International Journal of Eating Disorders

Assessing Fears of Negative Consequences in Children With Symptoms of Avoidant Restrictive Food Intake Disorder

Article

Author: Bryant‐Waugh, Rachel ; Rivera‐Cancel, Alannah M. ; LeMay‐Russell, Sarah ; Sapiro, Guillermo ; Lachman, Sage ; Loeb, Katharine L. ; Mines, Ellen V. ; Katzman, Debra K. ; Nicholas, Julia ; Marsan, Samuel ; Jackson, Jalisa E. ; Pilato, Ilana ; Zucker, Nancy L. ; Kim, Young Kyung ; Di Martino, J. Matias ; Gianneschi, Julia R. ; Marcus, Marsha D. ; Washington, Kara A. ; Pendergast, Jane

ABSTRACTObjectiveFear of Aversive Consequences (FOAC), such as choking or vomiting, is an important associated feature of Avoidant/Restrictive Food Intake Disorder (ARFID). However, the manifestation of FOAC in young children is poorly understood. This study aimed to describe the fears of children with ARFID symptoms and examine the concordance between parent and child ratings of fear.MethodChild‐reported FOAC was assessed using an interview designed for children between 6 and 10 years old, the Gustatory Avoidance and Gastrointestinal Stress Symptoms (GAGSS). Parents were administered a semi‐structured diagnostic interview regarding their child's symptoms, the Pica, ARFID, and Rumination Interview.ResultsAmong 68 children with ARFID diagnoses or symptoms (41.2% female, 85.3% White, mean age = 8.2 years, SD = 1.1 years; range 5.2–9.9 years), 91.2% of children endorsed at least one fear relative to 26.5% of parents. Among parent–child dyads, 36.8% disagreed about the child's fear of stomach pain (κ = 0.12) and 48.5% disagreed about the child's fear of vomiting, (κ = 0.08), both indicating low inter‐rater reliability. On average, children endorsed 4.3 (SD = 2.3) fears out of 9 options. The most frequently endorsed fears were that food will “taste bad,” (n = 43, 63.2%), “make you gag” (n = 37, 54.4%), and “look disgusting” (n = 36, 52.9%).DiscussionFindings highlight ways in which fear may manifest in children with ARFID that are not easily discernable by adults. Greater precision in depicting childhood fears may facilitate the earlier detection of problematic eating behaviors.

01 Mar 2021·Combinatorial Chemistry & High Throughput Screening

Discovery of Potent SARS-CoV-2 Inhibitors from Approved Antiviral Drugs via Docking and Virtual Screening

Article

Author: Chtita, Samir ; Bouachrine, Mohammed ; Aouidate, Adnane ; Belaidi, Salah ; Belhassan, Assia ; Lakhlifi, Tahar

Background:Coronavirus Disease 2019 (COVID-19) pandemic continues to threaten patients, societies and healthcare systems around the world. There is an urgent need to search for possible medications.Objective:This article intends to use virtual screening and molecular docking methods to find potential inhibitors from existing drugs that can respond to COVID-19.Methods:To take part in the current research investigation and to define a potential target drug that may protect the world from the pandemic of corona disease, a virtual screening study of 129 approved drugs was carried out which showed that their metabolic characteristics, dosages used, potential efficacy and side effects are clear as they have been approved for treating existing infections. Especially 12 drugs against chronic hepatitis B virus, 37 against chronic hepatitis C virus, 37 against human immunodeficiency virus, 14 anti-herpesvirus, 11 anti-influenza, and 18 other drugs currently on the market were considered for this study. These drugs were then evaluated using virtual screening and molecular docking studies on the active site of the (SARS-CoV-2) main protease (6lu7). Once the efficacy of the drug is determined, it can be approved for its in vitro and in vivo activity against the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), which can be beneficial for the rapid clinical treatment of patients.:These drugs were considered potentially effective against SARS-CoV-2 and those with high molecular docking scores were proposed as novel candidates for repurposing. The N3 inhibitor cocrystallized with protease (6lu7) and the anti-HIV protease inhibitor Lopinavir were used as standards for comparison.Results:The results suggest the effectiveness of Beclabuvir, Nilotinib, Tirilazad, Trametinib and Glecaprevir as potent drugs against SARS-CoV-2 since they tightly bind to its main protease.Conclusion:These promising drugs can inhibit the replication of the virus; hence, the repurposing of these compounds is suggested for the treatment of COVID-19. No toxicity measurements are required for these drugs since they were previously tested prior to their approval by the FDA. However, the assessment of these potential inhibitors as clinical drugs requires further in vivo tests of these drugs.

01 Jan 2018·MaturitasQ3 · MEDICINE

The male-female health-survival paradox in hospitalised older adults

Q3 · MEDICINE

Article

Author: Peel, Nancye M ; Hubbard, Ruth E ; Gordon, Emily H

OBJECTIVESTo determine whether the 'male-female health-survival paradox' is present in older hospitalised adults and to examine whether sex differences in the 'lethality' of acute medical conditions influence the relationship between sex and mortality.STUDY DESIGN AND OUTCOME MEASURESThis study was a secondary analysis of prospective cohort data collected from 1418 Australian inpatients aged 70 years and over. Frailty was measured using a 39-variable Frailty Index (FI-AC). Analyses examined the relationship between sex, age, FI-AC and 28-day mortality. Survival models were adjusted for 'lethality' of acute conditions (high versus low mortality risk).RESULTSThe FI-AC had a normal distribution in both sexes (female mean=0.34 (±0.13); male mean=0.31 (±0.15)). When adjusted for age, females had similar FI-AC scores to males (β coefficient=0.014, 95% confidence interval (CI)=0.00-0.028, p=0.056). There were 80 deaths in the sample, with females facing a significantly lower mortality risk than males of the same FI-AC and age (HR=0.39, 95% CI=0.25-0.63, p<0.001). Females were less likely than males to be admitted with a high-risk acute condition. Even so, this did not significantly reduce their survival advantage (HR=0.46, 95% CI=0.29-0.73, p=0.001).CONCLUSIONThe male-female health-survival paradox was not demonstrated in this study of older inpatients. Whilst females faced a significantly lower risk of near-term mortality, the sexes were found to have similar levels of frailty on admission to hospital. The sex mortality gap was not explained by sex differences in the 'lethality' of acute medical conditions.

100 Deals associated with Fiacitabine

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External Link

KEGG	Wiki	ATC	Drug Bank
D04180	-	-	DB12901

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Cytomegalovirus Infections	Phase 2	-	Memorial Sloan Kettering Cancer Center	-
Cytomegalovirus Infections	Phase 2	-	Allergan UC	-
Cytomegalovirus Infections	Phase 2	-	Allergan UC	-
Cytomegalovirus Infections	Phase 2	-	Memorial Sloan Kettering Cancer Center	-
Herpes Simplex	Phase 2	United States	-	-
Herpes Simplex	Phase 2	-	Memorial Sloan Kettering Cancer Center	-
Herpes Simplex	Phase 2	-	Allergan UC	-