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Related Concept Videos

Preclinical Development: Overview01:28

Preclinical Development: Overview

Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance01:07

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
A recent model describes pravastatin's hepatobiliary excretion, mediated...
Pulmonary Embolism II: Diagnostic Studies and Interprofessional Care01:29

Pulmonary Embolism II: Diagnostic Studies and Interprofessional Care

Diagnosing Pulmonary EmbolismDiagnosing pulmonary embolism (PE) involves clinical assessment and advanced imaging tests. The preferred diagnostic tool is the spiral (helical) CT scan or CT angiography (CTA), which uses intravenous contrast media to visualize the pulmonary vasculature and identify emboli.A ventilation-perfusion (V/Q) scan is an alternative for patients unable to receive contrast media. This scan includes both perfusion and ventilation scanning. Perfusion scanning involves...
Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions01:15

Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions

PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure (CHF).

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Related Experiment Video

Updated: Jun 13, 2026

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
09:44

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Published on: January 29, 2019

Pralatrexate - from bench to bedside.

Jasmine M Zain1, E Marchi

  • 1New York University Cancer Institute, NYU Langone Medical Center, New York, NY 10016, USA. jasmine.zain@nyumc.org

Drugs of Today (Barcelona, Spain : 1998)
|April 16, 2010
PubMed
Summary

Pralatrexate, a novel antifolate chemotherapy, shows promise for T-cell lymphomas and lung cancer. Its targeted delivery via RFC-1 enhances cellular uptake and antitumor effects, marking a significant advancement in cancer treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Development

Background:

  • Pralatrexate (PDX) is a new antifolate chemotherapy agent.
  • It demonstrates significant activity in T-cell lymphomas and non-small cell lung cancer.
  • Pralatrexate is FDA-approved for relapsed/refractory peripheral T-cell lymphomas (PTCL).

Purpose of the Study:

  • To detail the development of Pralatrexate from research to clinical application.
  • To highlight Pralatrexate's mechanism of action and therapeutic potential.

Main Methods:

  • Review of Pralatrexate's design and preclinical studies.
  • Analysis of clinical trial data and FDA approval process.

Main Results:

  • Pralatrexate exhibits high affinity for the folate carrier (RFC-1), improving cellular internalization.

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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader

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Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
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Published on: May 24, 2024

  • This enhanced uptake leads to greater antitumor efficacy compared to methotrexate.
  • Successful FDA approval for PTCL treatment underscores its clinical value.
  • Conclusions:

    • Pralatrexate represents a significant advancement in antifolate chemotherapy.
    • Its targeted mechanism offers improved efficacy in specific cancer types.
    • The drug's development journey illustrates successful bench-to-bedside translation.