Delving into the Latest Updates on Apricitabine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(-)dOTC, ATC

+ [4]

Target

RT

Mechanism

RT inhibitors(Reverse transcriptase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV Infections

Originator Organization

Shire Pharmaceuticals Services Ltd.

Active Organization-

Inactive Organization

Avexa LLC

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

Structure

Molecular FormulaC8H11N3O3S

InChIKeyRYMCFYKJDVMSIR-RNFRBKRXSA-N

CAS Registry160707-69-7

This study will examine the long term safety of apricitabine in HIV-1 infected patients from studies AVX-301 or AVX-302. Eligible patients are those who have either (a)completed studies AVX-301 or AVX-302; or (b)met the criteria for virological failure/lack of response, and consequently wish to withdraw early from studies AVX-301 or AVX-302.

Start Date01 May 2008

Sponsor / Collaborator

Avexa LLC

NCT00612898 / TerminatedPhase 2/3

A Phase 2b/3, Randomized, Double Blind, Dose Confirming Study of the Safety, Efficacy and Tolerability of Apricitabine Versus Lamivudine in Treatment-experienced HIV-1 Infected Patients With the M184V/I Mutation in Reverse Transcriptase

Apricitabine is a new NRTI which is active against drug-resistant HIV. NRTIs are often included as part of patients' treatment, but many HIV-infected patients develop resistance to commonly used NRTIs such as lamivudine (3TC) and emtricitabine (FTC). This study will examine whether including apricitabine as part of patients' treatment is more effective than including lamivudine,when patients change treatment because of drug resistance.

Start Date01 Feb 2008

Sponsor / Collaborator

Avexa LLC

ACTRN12606000443594 / CompletedPhase 2

An open label extension study to evaluate the long term safety and efficacy of apricitabine in controlling Human Immunodeficiency Virus (HIV) viral load and disease progression in treatment-experienced HIV-1 infected subjects

Start Date01 Sep 2006

Sponsor / Collaborator-

100 Clinical Results associated with Apricitabine

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100 Translational Medicine associated with Apricitabine

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100 Patents (Medical) associated with Apricitabine

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268

Literatures (Medical) associated with Apricitabine

09 Aug 2024·Antioxidants (Basel, Switzerland)

Effects of Acremonium terricola Culture on Lactation Performance, Immune Function, Antioxidant Capacity, and Intestinal Flora of Sows.

Article

Author: Chen, Qiangqiang ; Sun, Qian ; Hua, Weidong ; Xiao, Lixia ; Chen, Zhirong ; Zhang, Jinzhi

This study aimed to determine the effects of different doses of Acremonium terricola culture (ATC) on lactation performance, immune function, antioxidant capacity, and intestinal flora of sows. Forty-five Landrace sows (3-6 parity) were randomly assigned to the following three treatments from 85 days of gestation to 21 days after farrowing: a control diet (CON, basal diet), a low-dose Acremonium terricola culture diet (0.2% ATC, basal diet + 0.2% ATC), and a high-dose Acremonium terricola culture diet (0.4% ATC, basal diet + 0.4% ATC). Compared with the CON group, the supplementation of 0.2% ATC increased the average daily milk yield of sows by 4.98%, increased milk fat, total solids, and freezing point depression on day 1 postpartum (p < 0.05), increased serum concentration of Triiodothyronine, Thyroxin, and Estradiol on day 21 postpartum (p < 0.05). Compared with the CON group, the supplementation of 0.4% ATC increased the average daily milk yield of sows by 9.38% (p < 0.05). Furthermore, the supplementation of 0.2% ATC increased serum concentration of IgG, IgM, and IFN-γ, CD4 on day 1 postpartum (p < 0.05) and increased serum concentration of immunoglobulin A ( IgA), immunoglobulin G (IgG), immunoglobulin M ( IgM), complement 3 (C3), cluster of differentiation 4 (CD4), cluster of differentiation 8 (CD8), interferon-γ (IFN-γ) on day 21 postpartum (p < 0.05), while the supplementation of 0.4% ATC reduced serum concentration of IL-2 on day 21 postpartum (p < 0.05). Moreover, the supplementation of 0.4% ATC significantly increased serum concentration of catalase (CAT) (p < 0.05). Additionally, the supplementation of ATC affected the relative abundance of the intestinal flora at different taxonomic levels in sows and increased the abundance of beneficial bacteria such as in the norank_f__Eubacterium_coprostanoligenes group, Eubacterium_coprostanoligenes group, and Lachnospiraceae_XPB1014 group of sows, while reducing the abundance of harmful bacteria such as Phascolarctobacterium and Clostridium_sensu_stricto_1. These data revealed that the supplementation of ATC during late gestation and lactation can improve lactation performance, immune function, antioxidant capacity, and the gut microbiota. Compared with supplementation of 0.4% ATC, 0.2% ATC enhances the levels of thyroid-related hormones, specific antibodies, and cytokines in serum, promotes the diversity of beneficial gut microbiota, beneficial bacteria in the intestine, reduces the population of harmful bacteria, and thereby bolsters the immunity of sows. Hence, 0.2% ATC is deemed a more optimal concentration.

01 Aug 2024·Cancer Research

The DNA Methyltransferase Inhibitor 5-Aza-4′-thio-2′-Deoxycytidine Induces C>G Transversions and Acute Lymphoid Leukemia Development

Article

Author: Aplan, Peter D. ; Bertoli, Ryan M. ; Meltzer, Paul S. ; Klimaszewski, Haley ; Walter, Matthew J. ; Zhu, Yuelin J. ; Marasco, Madison R.B. ; Wokasch, Anthony ; Khanna, Ajay ; Gammell, Susannah ; Doroshow, James H. ; Cao, Dengchao ; Difilippantonio, Michael J. ; Chung, Yang Jo ; Walker, Robert L.

AbstractDNA methyltransferase inhibitors (DNMTi), most commonly cytidine analogs, are compounds that decrease 5′-cytosine methylation. DNMTi are used clinically based on the hypothesis that cytosine demethylation will lead to re-expression of tumor suppressor genes. 5-Aza-4′-thio-2′-deoxycytidine (Aza-TdCyd or ATC) is a recently described thiol-substituted DNMTi that has been shown to have anti-tumor activity in solid tumor models. In this study, we investigated the therapeutic potential of ATC in a murine transplantation model of myelodysplastic syndrome. ATC treatment led to the transformation of transplanted wild-type bone marrow nucleated cells into lymphoid leukemia, and healthy mice treated with ATC also developed lymphoid leukemia. Whole-exome sequencing revealed 1,000 acquired mutations, almost all of which were C>G transversions in a specific 5′-NCG-3′ context. These mutations involved dozens of genes involved in human lymphoid leukemia, such as Notch1, Pten, Pax5, Trp53, and Nf1. Human cells treated in vitro with ATC showed 1,000 acquired C>G transversions in a similar context. Deletion of Dck, the rate-limiting enzyme for the cytidine salvage pathway, eliminated C>G transversions. Taken together, these findings demonstrate a highly penetrant mutagenic and leukemogenic phenotype associated with ATC.Significance: Treatment with a DNA methyltransferase inhibitor generates a distinct mutation signature and triggers leukemic transformation, which has important implications for the research and clinical applications of these inhibitors.

01 Jul 2024·Reviews in Medical Virology

Efficacy and safety of adoptive T‐cell therapy in treating cytomegalovirus infections post‐haematopoietic stem cell transplantation: A systematic review and meta‐analysis

Review

Author: Ahmadvand, Mohammad ; Taherian, Mohammad Reza ; Daneshvar, Alireza ; Toufani, Shahin ; Barkhordar, Maryam ; Aliabadi, Leyla Sharifi ; Yaghmaie, Marjan ; Vaezi, Mohammad ; Bahri, Tanaz ; Azarbar, Pouya

AbstractCytomegalovirus (CMV) infection poses significant risks in allogeneic haematopoietic stem cell transplant (allo‐HSCT) recipients. Despite advances in antiviral therapies, issues such as drug resistance, side effects, and inadequate immune reconstitution remain. This systematic review and meta‐analysis aim to evaluate the efficacy and safety of adoptive cell therapy (ATC) in managing CMV infections in allo‐HSCT recipients. Adhering to preferred reporting items for systematic reviews and meta‐analyses guidelines, we conducted a comprehensive database search through July 2023. A systematic review and meta‐analysis were conducted on studies involving HSCT patients with CMV infections treated with ATC. The primary outcome was the response rate to ATC, and secondary outcomes included adverse events associated with ATC. The Freeman–Tukey transformation was applied for analysis. In the meta‐analysis of 40 studies involving 953 participants, ATC achieved an overall integrated response rate of 90.16%, with a complete response of 82.59% and a partial response of 22.95%. ATC source, HLA matching, steroid intake, and age group markedly influenced response rates. Donor‐derived T‐cell treatments exhibited a higher response rate (93.66%) compared to third‐party sources (88.94%). HLA‐matched patients demonstrated a response rate of 92.90%, while mismatched patients had a lower rate. Children showed a response rate of 83.40%, while adults had a notably higher rate of 98.46%. Adverse events were minimal, with graft‐versus‐host disease occurring in 24.32% of patients. ATC shows promising response rates in treating CMV infections post‐HSCT, with an acceptable safety profile. However, to establish its efficacy conclusively and compare it with other antiviral treatments, randomised controlled trials are essential. Further research should prioritise such trials over observational and one‐arm studies to provide robust evidence for clinical decision‐making.

1

News (Medical) associated with Apricitabine

04 Jun 2009

·www.biospace.com

Positive Outcome Reached at 16 Weeks for Avexa Limited's ATC Phase III Trial

MELBOURNE, Australia--(BUSINESS WIRE)--Avexa Limited (ASX:AVX) announced that the Data Safety Monitoring Board (DSMB) met today to review the 16 week data from Avexa’s apricitabine (ATC) Phase III clinical trial. The DSMB reviewed the data and recommended continuation of the study with the 800mg dose. Patients taking the 1200mg dose will be transitioned to the optimum 800mg dose to continue their therapy.

100 Deals associated with Apricitabine

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Apricitabine	J05AB	DB12855

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Phase 3	IL	Avexa LLC	01 Feb 2008
HIV Infections	Phase 3	CA	Avexa LLC	01 Feb 2008
HIV Infections	Phase 3	DE	Avexa LLC	01 Feb 2008
HIV Infections	Phase 3	GB	Avexa LLC	01 Feb 2008
HIV Infections	Phase 3	AU	Avexa LLC	01 Feb 2008
HIV Infections	Phase 3	US	Avexa LLC	01 Feb 2008
HIV Infections	Phase 3	IT	Avexa LLC	01 Feb 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


IAS2008	Not Applicable	HIV Infections	51	Apricitabine 600mg	(mhoxomtgqz) = sxiylgiite anjywznqza (pkrmwblriu ) View more	-	01 Jan 2008
				Apricitabine 800mg	(mhoxomtgqz) = nbuydxzdqy anjywznqza (pkrmwblriu ) View more
IAS2006	Not Applicable	HIV Infections	-	apricitabine (HIV- subjects)	fnwedwyoas(bsgnuzblta) = ainkqdkyhf xmebsbkxfm (fmjaodukhg ) View more	-	01 Jan 2006
				apricitabine (HIV+ subjects)	fnwedwyoas(bsgnuzblta) = oncxsdobxa xmebsbkxfm (fmjaodukhg ) View more
IAS2003	Not Applicable	HIV Infections	63	SPD754 400mg	zxbkcblxhr(jltpvotwnu) = ldwvebzcuu neamuccdys (yfoezvaqyk )	Positive	01 Jan 2003
				SPD754 800mg	zxbkcblxhr(jltpvotwnu) = gzuufrdnrb neamuccdys (yfoezvaqyk )
BCH-10618 (IAS2001)	Not Applicable	-	-	BCH-10618	qnkaqxyjqx(uiyexfcxmv) = rssnzrdagr xdvjnzbikw (igirruypne ) View more	-	01 Jan 2001