Delving into the Latest Updates on Ximelagatran with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ximelagatran (JAN/USAN/INN)

+ [2]

Target

thrombin

Action

inhibitors

Mechanism

thrombin inhibitors(Factor IIa inhibitors)

Therapeutic Areas

Cardiovascular DiseasesOther DiseasesNervous System Diseases

Active Indication-

Inactive Indication

Atrial FibrillationHip FracturesStroke+ [1]

Originator Organization

AstraZeneca PLC

Active Organization

AstraZeneca India Pvt Ltd.

Inactive Organization

AstraZeneca PLC

Drug Highest PhaseApproved

First Approval Date

France (05 May 2004)

Regulation-

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Structure/Sequence

Molecular FormulaC24H35N5O5

InChIKeyZXIBCJHYVWYIKI-PZJWPPBQSA-N

CAS Registry192939-46-1

The "EXTEND" Study: A Randomized, Double-blind, Parallel-group, Phase III b, Multi-centre Study Evaluating Extended Prophylactic Treatment With Melagatran/Ximelagatran Versus Enoxaparin for the Prevention of Venous Thromboembolic Events in Patients Undergoing Elective Hip Replacement or Hip Fracture Surgery.

This study is being carried out to study the efficacy and safety of treatment with melagatran injection followed by ximelagatran tablets in preventing blood clots, compared with enoxaparin for a period of 5-6 weeks. A separate visit, independent from the study will be done approximately 6 months after the surgery.

Start Date01 Sep 2005

Sponsor / Collaborator

AstraZeneca PLC

EUCTR2004-002746-35-AT

/ Not yet recruitingNot Applicable

The EXTEND study: A randomized, double-blind, parallel-group, phase IIIb, multi-centre study evaluating extended prophylactic treatment with melagatran/ximelagatran versus enoxaparin for the prevention of venous thromboembolic events in patients undergoing elective hip replacement or hip fracture surgery. - EXTEND

Start Date19 Jul 2005

Sponsor / Collaborator

AstraZeneca AB

NCT00206063

/ TerminatedPhase 2

Long-Term Treatment With the Oral Direct Thrombin Inhibitor Ximelagatran, Compared to Warfarin, as Stroke Prophylaxis in Patients With Atrial Fibrillation. A Long Term Follow-Up Study

The purpose of this study is to evaluate tolerability of long-term treatment with ximelagatran compared to standard treatment with warfarin.

Start Date01 Aug 1999

Sponsor / Collaborator

AstraZeneca PLC

100 Clinical Results associated with Ximelagatran

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100 Translational Medicine associated with Ximelagatran

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100 Patents (Medical) associated with Ximelagatran

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680

Literatures (Medical) associated with Ximelagatran

01 Jun 2024·Exploratory Research in Clinical and Social Pharmacy

Incidence of drug-related adverse events related to the use of high-alert drugs: A systematic review of randomized controlled trials

Review

Author: Silvestre, Carina Carvalho ; de Oliveira Filho, Alfredo Dias ; Valença-Feitosa, Fernanda ; Lobo, Iza Maria Fraga ; Menezes, Michelle Santos ; Doria, Grace Anne Azevedo ; Pereira, Sylmara Nayara ; Quintans-Júnior, Lucindo José

BackgroundHigh-alert medication (HAM) is more predictable to cause significant harm to the patient, even when used as intended. The damage related to the HAM lead not only suffering to the patient, but also raise the additional costs associated with care.ObjectiveEvaluate the incidence of drug-related adverse events related to the use of high-alert medications.MethodsIt was conducted an active search for information through COCHRANE databases, LILACS, SciELO, SCOPUS, PubMed/MEDLINE and WEB OF SCIENCE. The search strategy included the following terms: "Patient safety", "Medication errors" and "Hospital" and "High Alert Medications" or "Dangerous Drugs" in different combinations. Then two reviewers independently conducted a preliminary evaluation of relevant titles, abstracts and finally full-text. Studies quality was evaluated according to PRISMA declaration.ResultsThe systematic review evaluated seven articles, which showed that only 11 HAM identified in the literature could have serious events. The most frequently cited were warfarin (22.2%) which progressed from deep vein thrombosis to gangrene, suggesting lower initial doses, followed by cyclophosphamide (22.2%) and cyclosporine (22.2%) which presented invasive fungal infection and death. In addition to these, morphine was compared with its active metabolite (M6G), with M6G causing fewer serious clinical events related to nausea and vomiting, reducing the need for concomitant use of antiemetics.ConclusionsThe most reported drug classes in the articles included that were related to incidence of drug-related adverse events in use of high-alert medications: morphine, M6G-glucuronide, haloperidol, promethazine, ivabradine, digoxin, warfarin, ximelagatran, cyclophosphamide, cyclosporine, and ATG. The formulate protocols for the use of these medications, with importance placed on evaluating, among the classes, the medication that causes the least harm.

29 Apr 2024·Cureus

Effectiveness of Anticoagulants in Reducing Stroke Risk Among Patients With Atrial Fibrillation

Review

Author: Bodduluri, Monicaa ; Valiveti, Sindhu Chowdary ; Gadde, Sai T ; Dasari, Sai Namrata ; Myneni, Pravallika

Atrial fibrillation (AF) is a type of cardiac arrhythmia causing shortness of breath, lightheadedness, and palpitations. It may go unrecognized and asymptomatic among many patients. AF is not a potentially fatal arrhythmia; its hemodynamic, structural, and hemocoagulative effects have a significant impact on the standard of life, which can lead to various complications such as stroke. A stroke caused by AF leads to additional burdens on both patients and the global economy. Patients with AF can prevent strokes with oral anticoagulants; however, ensuring diligent adherence to medication is crucial for maximizing treatment efficacy. Since they have a lighter treatment load than warfarin, non-vitamin K antagonist oral anticoagulants (NOACs) are also recommended with better hope for medication adherence. Various anticoagulants such as warfarin and ximelagatran, among many more, are prescribed to patients who have the potential to reduce the incidence of stroke as well as alleviate their likelihood of developing other thromboembolic events that can decrease their quality of life. Economic and psychological burdens associated with diminished functionality can be prevented by anticoagulant therapy among AF patients, therefore reducing their economic and social burden. This is due to the negative association between stroke among AF patients and anticoagulation consumption.

04 Dec 2023·Molecular Pharmaceutics

Approaches to Account for Colon Absorption in Physiologically Based Biopharmaceutics Modeling of Extended-Release Drug Products

Article

Author: Jadhav, Harshad ; Augustijns, Patrick ; Tannergren, Christer

The rate and extent of colon absorption are important determinants of the in vivo performance of extended-release (ER) drug products. The ability to appropriately predict this at different stages of development using mechanistic physiologically based biopharmaceutic modeling (PBBM) is highly desirable. This investigation aimed to evaluate the prediction performance of three different approaches to account for colon absorption in predictions of the in vivo performance of ER drug product variants with different in vitro release profiles. This was done by mechanistic predictions of the absorption and plasma exposure of the ER drug products using GastroPlus and GI-Sim for five drugs with different degrees of colon absorption limitations in humans. Colon absorption was accounted for in the predictions using three different approaches: (1) by an a priori approach using the default colon models, (2) by fitting the colon absorption scaling factors to the observed plasma concentration-time profiles after direct administration to the colon in humans, or (3) from the ER drug product variant with the slowest in vitro release profile. The prediction performance was evaluated based on the percentage prediction error and the average absolute prediction error (AAPE). Two levels of acceptance criteria corresponding to highly accurate (AAPE ≤ 20%) and accurate (AAPE 20-50%) predictions were defined prior to the evaluation. For the a priori approach, the relative bioavailability (F_rel), AUC_0-t, and C_max of the ER drug product variants for the low to medium colon absorption limitation risk drugs was accurately predicted with an AAPE range of 11-53 and 8-59% for GastroPlus and GI-Sim, respectively. However, the prediction performance was poor for the high colon absorption limitation risk drugs. Moreover, accounting for the human regional colon absorption data in the models did not improve the prediction performance. In contrast, using the colon absorption scaling factors derived from the slowest ER variant significantly improved the prediction performance regardless of colon absorption limitation, with a majority of the predictions meeting the high accuracy criteria. For the slowest ER approach, the AAPE ranges were 5-24 and 5-32% for GastroPlus and GI-Sim, respectively, excluding the low permeability drug. In conclusion, the a priori PBBM can be used during candidate selection and early product design to predict the in vivo performance of ER drug products for low to medium colon absorption limitation risk drugs with sufficient accuracy. The results also indicate a limited value in performing human regional absorption studies in which the drug is administered to the colon as a bolus to support PBBM development for ER drug products. Instead, by performing an early streamlined relative bioavailability study with the slowest relevant ER in vitro release profile, a highly accurate PBBM suitable for ER predictions for commercial and regulatory applications can be developed, except for permeability-limited drugs.

100 Deals associated with Ximelagatran

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External Link

KEGG	Wiki	ATC	Drug Bank
D01981	Ximelagatran	B01AE05	DB04898

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Thromboembolism	Discovery	Austria	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Netherlands	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Finland	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Norway	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Mexico	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Belgium	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Portugal	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Hungary	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Sweden	AstraZeneca PLC	01 Sep 2005
Thromboembolism	Discovery	Germany	AstraZeneca PLC	01 Sep 2005