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Related Concept Videos

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Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
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Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
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Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Related Experiment Video

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Ponatinib: A comprehensive drug profile.

Mohamed W Attwa1, Hamad M Alkahtani2, Adel S El-Azab2

  • 1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia; Students' University Hospital, Mansoura University, Mansoura, Egypt.

Profiles of Drug Substances, Excipients, and Related Methodology
|February 29, 2024
PubMed
Summary

This review covers the synthesis, properties, and analysis of ponatinib, a tyrosine kinase inhibitor for treating resistant blood cancers like Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) and chronic myeloid leukemia (CML). It details characterization methods and explores non-compendial analytical techniques and pharmacokinetic studies.

Keywords:
Anticancer drugChromatographicImpuritiesPharmacologyPhysical and chemical characteristicPonatinibPreparation methodSpectroscopyTyrosine kinase inhibitorsUses and applications

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Analytical Chemistry

Background:

  • Ponatinib is a tyrosine kinase inhibitor crucial for treating resistant Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) and chronic myeloid leukemia (CML).
  • Understanding its synthesis, properties, and analytical methods is vital for effective therapeutic application.

Approach:

  • This chapter reviews existing literature on ponatinib synthesis and physicochemical properties.
  • It details structural characterization using techniques like NMR, MS, and XRD.
  • A comprehensive survey of non-compendial analytical methods (spectroscopic, chromatographic, immunoassay) and pharmacokinetic/pharmacodynamic studies is presented.

Key Points:

  • Synthesis and physicochemical properties of ponatinib are elucidated.
  • Various analytical techniques for ponatinib characterization are discussed, including spectroscopic and chromatographic methods.
  • Pharmacological and biochemical aspects, including pharmacokinetics and pharmacodynamics, are surveyed.

Conclusions:

  • This review consolidates knowledge on ponatinib's synthesis, characterization, and analysis.
  • It highlights the need for robust analytical methods for this important anti-cancer drug.
  • The findings support further research into ponatinib's therapeutic potential and application.