Apo-Imatinib

Country: New Zealand

Language: English

Source: Medsafe (Medicines Safety Authority)

Active ingredient:

Imatinib mesilate 119.5mg equivalent to Imatinib 100 mg

Available from:

Apotex NZ Ltd

INN (International Name):

Imatinib mesilate 119.5 mg (= Imatinib 100 mg)

Dosage:

100 mg

Pharmaceutical form:

Film coated tablet

Composition:

Active: Imatinib mesilate 119.5mg equivalent to Imatinib 100 mg Excipient: Colloidal silicon dioxide Crospovidone Hyprolose Hypromellose Iron oxide red Iron oxide yellow Macrogol 8000 Magnesium stearate

Prescription type:

Prescription

Manufactured by:

Apotex Pharmachem Inc

Therapeutic indications:

Treatment of adult and paediatric patients with newly diagnosed Philadelphia chromosome positive chronic myeloid leukaemia (Ph+CML). Treatment of adult and paediatic patients with Ph+CML in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy.

Product summary:

Package - Contents - Shelf Life: Blister pack, Alu/Alu cold form in outer cardboard carton - 20 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Blister pack, Alu/Alu cold form in outer cardboard carton - 30 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Blister pack, Alu/Alu cold form in outer cardboard carton - 60 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Blister pack, Alu/Alu cold form in outer cardboard carton - 90 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Blister pack, Alu/Alu cold form in outer cardboard carton - 100 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Bottle, 75cc round, white, opaque HDPE with blue PP child resistant cap and desiccant - 30 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Bottle, 75cc round, white, opaque HDPE with blue PP child resistant cap and desiccant - 60 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Bottle, 75cc round, white, opaque HDPE with blue PP screw cap and desiccant - 90 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture - Bottle, 75cc round, white, opaque HDPE with blue PP screw cap and desiccant - 100 tablets - 36 months from date of manufacture stored at or below 25°C protect from light and moisture

Authorization date:

2012-05-24

Summary of Product characteristics

NEW ZEALAND DATA SHEET
APO-IMATINIB
IMATINIB 100MG AND 400MG TABLETS
Please refer to Medsafe website (www.medsafe.govt.nz) for the most
recent datasheet
Page 1
PRESENTATION
Apo-Imatinib
100mg:
Brownish
orange,
round
biconvex,
bevelled-edge,
film-coated
tablets. Engraved “IMA” over score “100” on one side,
“APO” on the other side.
Apo-Imatinib 400mg: Brownish orange, capsule shaped biconvex
film-coated tablets.
Engraved “IMA” score “400” on one side, “APO” on the other
side.
USES
ACTIONS
Imatinib mesilate referred further as “imatinib” is a
protein-tyrosine kinase inhibitor, which
potently inhibits the breakpoint cluster region-Abelson (Bcr-Abl)
tyrosine kinase at the in
vitro, cellular, in vivo levels.
The compound selectively inhibits proliferation and induces apoptosis
in Bcr-Abl positive
cell lines as well as fresh leukaemic cells from Philadelphia
chromosome positive CML
and acute lymphoblastic leukaemia (ALL) patients. In colony
transformation assays
using ex vivo peripheral blood and bone marrow samples, imatinib shows
selective
inhibition of Bcr-Abl positive colonies from CML patients.
_In vivo _ the compound shows anti-tumour activity as a single agent
in animal models
using Bcr-Abl positive tumour cells.
Imatinib is also an inhibitor of the receptor tyrosine kinases for
platelet-derived growth
factor (PDGF) and stem cell factor (SCF), c-Kit, and inhibits PDGF-
and SCF-mediated
cellular
events.
_In _
_vitro_,
imatinib
inhibits
proliferation
and
induces
apoptosis
in
gastrointestinal stromal tumour (GIST) cells, which express an
activating kit mutation.
Constitutive
activation
of
the
PDGFR
or
the
Abl
protein
tyrosine
kinases
as
a
consequence of fusion to diverse partner proteins or constitutive
production of PDGF
have been implicated in the pathogenesis of MDS/MPD, HES/CEL and DFSP.
In
addition, constitutive activation of c-Kit or the PDGFR has been
implicated in the
pathogenesis of SM. Imatinib inhibits signalling and proliferation of
cells driven by
dysregulated PDGFR, Kit and