Imatinib Grindex hard capsules 100 mg. №120

Description

Imatinib Grindex Storage
active substance: imatinib;

1 hard capsule contains 100 mg of imatinib (as imatinib mesylate);

excipients: prosolv (microcrystalline cellulose, colloidal anhydrous silica), crospovidone, talc, magnesium stearate;

capsule (body and lid): iron oxide red (E 172), iron oxide yellow (E 172), titanium dioxide (E 171), gelatin.

Imatinib Grindex Dosage form
Hard capsules.

Main physical and chemical properties: hard gelatin capsules of brown-orange color. Capsule content – powder from white to light yellow or brownish-yellow color.

Imatinib Grindex Pharmacotherapeutic group
Other antineoplastic agents. Protein kinase inhibitor.

ATX code L01X E01.

Pharmacological properties

Pharmacodynamics.

Imatinib is a protein tyrosine kinase inhibitor that strongly inhibits Bcr-Abl tyrosine kinase in vitro, at the cellular and in vivo levels. This compound selectively inhibits proliferation and stimulates apoptosis in Bcr-Abl-positive cell lines, as well as in newly affected leukemic cells in patients with the presence of Philadelphia chromosome in leukocytes in chronic positive myelogenous leukemia (Rh + leukolemia) and

In vivo, the compound exhibits antitumor activity in monotherapy in a model of Bcr-Abl-positive tumor cells in animals. In addition, imatinib is a potent inhibitor of platelet-derived tyrosine kinase receptor (TGF) and embryonic cell factor (FEC), c-Kit, and inhibits TGF- and FEC-mediated cell changes. In vitro, imatinib inhibits proliferation and stimulates apoptosis in cells of the gastrointestinal stromal tumor (GIST), which is expressed in the activation of the kit mutation.

Indication
Treatment of patients (adults and children) with newly diagnosed positive (Ph +) (with the presence of Philadelphia chromosome (bcr-abl) in leukocytes) chronic myeloid leukemia (CML), for whom bone marrow transplantation is not considered as the first line of therapy;
treatment of patients (adults and children) with (Ph + CML) in the chronic phase after unsuccessful interferon alpha therapy or in the acceleration phase, or in the blast crisis phase of the disease;
as part of chemotherapy in adult patients with newly diagnosed positive acute lymphoblastic leukemia (Ph + GLL) with the presence of philadelphia chromosome in leukocytes;
as monotherapy in adult patients with acute lymphoblastic leukemia (Ph + GLL) in relapse or difficult to treat;
treatment of adult patients with myelodysplastic / myeloproliferative diseases (MDS / MPZ) associated with platelet growth factor receptor (FRT) gene rearrangement;
treatment of adults with hypereosinophilic syndrome (HES) and / or chronic eosinophilic leukemia (CHL) with rearrangement of FIP1L1-PDGFRα genes;
treatment of adult patients with Kit (CD117) -positive inoperable and / or metastatic malignant gastrointestinal stromal tumors (GIST);
adjuvant therapy in adult patients at high risk of recurrence of Kit (CD117) -positive malignant gastrointestinal stromal tumors (GIST) after resection (patients at low or minimal risk may not receive adjuvant therapy);
treatment of adult patients with inoperable protruding dermatofibrosarcoma (DESP) and adult patients with recurrent and / or metastatic dermatofibrosarcoma (DESP) who cannot be removed surgically.
The effect of imatinib on bone marrow transplantation has not been established.

In adults and children, the efficacy of imatinib is assessed on the basis of data on the frequency of general hematological and cytogenetic response and progression-free survival in CML, the frequency of hematological and cytogenetic response in Ph + GLL, MDS / MPZ, the frequency of hematological response in HES / HEL and the frequency of effective response in adult patients with inoperable and / or metastatic GIST and DFSP, as well as progression-free survival in adjuvant therapy of patients with GIST. Experience with imatinib in patients with MDS / MPZ associated with PDGFR gene rearrangement is very limited. With the exception of newly diagnosed CML in the chronic phase, controlled trials that would prove clinical benefit or increased survival have not been performed in these diseases.

Contraindication
Hypersensitivity to the active substance or to any of the excipients.