Description

Ibruxen (Ibrutinib) 140 mg is a generic drug used to treat certain types of blood cancer, including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). Each Ibruxen capsule contains 140 mg of the active ingredient ibrutinib. Ibruxen is a kinase inhibitor that works by blocking the activity of a protein called Bruton’s tyrosine kinase, which is involved in the growth and survival of cancer cells.The recommended dosage of Ibruxen is one 140 mg capsule taken orally once daily. Ibruxen is typically taken until the cancer progresses or unacceptable toxicity occurs. The product is available in bottles of 120 capsules.

Active Ingredient

• Ibruxen contains the active ingredient ibrutinib, which is a Bruton’s tyrosine kinase (BTK) inhibitor.

Indication

• Ibruxen is approved for the treatment of certain blood cancers, including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL).

Dosage

• The recommended dosage is one 140 mg capsule taken orally once daily.

Packaging

• Ibruxen is available in bottles of 120 capsules, providing a 120-day supply when taken as directed.

Manufacturer

• Ibruxen is a generic version of the brand-name drug Imbruvica, manufactured by a different pharmaceutical company.

Availability

• As a generic drug, Ibruxen may be more affordable than the brand-name Imbruvica for patients with certain insurance coverage or financial constraints.

Key Considerations

• Patients should follow their healthcare provider’s instructions carefully when taking Ibruxen and report any side effects or concerns.
• Ibruxen may interact with certain other medications, so patients should inform their healthcare provider of all medications they are taking.
• Regular monitoring and follow-up with the healthcare provider are important for patients taking Ibruxen.
  

  Key Benefits

  • Ibruxen is a kinase inhibitor used to treat certain types of blood cancer, including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL).
  • The active ingredient, ibrutinib, works by inhibiting the activity of an enzyme called Bruton’s tyrosine kinase (BTK). BTK plays a crucial role in the growth and survival of malignant B cells.
  • By blocking BTK, ibrutinib disrupts B cell receptor signaling and induces apoptosis (programmed cell death) in cancer cells, helping to stop the growth and spread of abnormal blood cells.
  • Ibruxen has demonstrated antineoplastic (anti-cancer) properties and is effective in slowing disease progression in certain blood cancers.

  Mechanism of Action

  • Ibrutinib binds covalently to a cysteine residue in the BTK active site, leading to irreversible inhibition of the enzyme.
  • This disrupts B cell receptor signaling and blocks the survival and proliferation of malignant B cells.
  • Ibrutinib has been shown to induce apoptosis in chronic lymphocytic leukemia (CLL) cells and inhibit the adhesion and migration of CLL cells.
  • Through its selective and irreversible inhibition of BTK, ibrutinib exerts its therapeutic effect in treating certain blood cancers.
    

    Chemical Structure

    The chemical structure of ibrutinib, the active ingredient in Ibruxen, is as follows:Ibrutinib chemical structureThe molecular formula of ibrutinib is C25H24N6O2, and its IUPAC name is 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]prop-2-en-1-one.

    Key Structural Features

    • Ibrutinib contains a pyrazolo[3,4-d]pyrimidine core structure, which is a key pharmacophore for kinase inhibition.
    • The piperidine ring and the phenoxyphenyl substituent contribute to the binding interactions with the Bruton’s tyrosine kinase (BTK) enzyme.
    • The acrylamide moiety forms a covalent bond with a cysteine residue in the BTK active site, leading to irreversible inhibition of the enzyme.
      

      Ring Structure

      • The core of the molecular structure of ibrutinib is a 6-5-membered, fused, heterocyclic ring system known as a dihydropurine ring. 
      • This dihydropurine ring can form hydrogen bonds with the Met477 residue in the active site of the Bruton’s tyrosine kinase (BTK) enzyme. 
      • The dihydropurine ring is a key pharmacophore, or structural feature, that allows ibrutinib to bind and inhibit the BTK enzyme. 
      • In addition to the dihydropurine core, ibrutinib’s structure also includes a piperidine ring and a phenoxyphenyl substituent, which contribute to the binding interactions with BTK. 
      • The acrylamide moiety on ibrutinib forms a covalent bond with a cysteine residue (C481) in the BTK active site, leading to irreversible inhibition of the enzyme.
        

        Key Aspects of Ibrutinib’s Ring Structure

        1. Dihydropurine Core: The core of ibrutinib’s molecular structure is a 6-5-membered, fused, heterocyclic ring system known as a dihydropurine ring. 
        2. Hydrogen Bonding: The dihydropurine ring can form hydrogen bonds with the Met477 residue in the active site of the BTK enzyme, allowing ibrutinib to bind and inhibit BTK. 
        3. Pharmacophore: The dihydropurine ring is a key pharmacophore, or structural feature, that enables ibrutinib to selectively bind and inhibit the BTK enzyme. 
        4. Covalent Binding: In addition to the dihydropurine core, ibrutinib’s structure includes an acrylamide moiety that forms a covalent bond with the Cys481 residue in the BTK active site, leading to irreversible inhibition of the enzyme. 
        5. Conformational Changes: Binding of ibrutinib to BTK induces conformational changes in the enzyme, including stabilization of the “αC-out” conformation, which disrupts the autoinhibited state of BTK and prevents its activation. 

        Dosage

        • The recommended dosage of Ibruxen (Ibrutinib) 140 mg for Mantle Cell Lymphoma (MCL) and Marginal Zone Lymphoma (MZL) is 560 mg (four 140 mg capsules) orally once daily until disease progression or unacceptable toxicity.
        • For Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) and Waldenstrom Macroglobulinemia (WM), the recommended dose is 420 mg (three 140 mg capsules) orally once daily until disease progression or unacceptable toxicity.
        • When used in combination with bendamustine and rituximab for CLL/SLL, the recommended dose of Ibruxen is also 420 mg (three 140 mg capsules) orally once daily until disease progression or unacceptable toxicity.

        Storage

        • Store Ibruxen 140 mg capsules below 30°C, protect from light, and keep out of reach of children.
        • Store in a dry place.

        Reviews

        • No reviews for Ibruxen 140 mg capsules were found in the search results.

        In summary, the dosage of Ibruxen 140 mg capsules varies depending on the specific indication, ranging from 420 mg to 560 mg taken orally once daily. The capsules should be stored below 30°C, protected from light, and kept in a dry place out of reach of children. No reviews were available for this product in the provided search results.