Axinix 1 Tablet

Nchi: Bangladeshi

Lugha: Kiingereza

Chanzo: DGDA (Directorate General of Drug Administration)

Viambatanisho vya kazi:

Axitinib

Inapatikana kutoka:

Beacon Pharmaceuticals PLC

INN (Jina la Kimataifa):

Axitinib

Kipimo:

1 mg

Dawa fomu:

Tablet

Tabia za bidhaa

COMPOSITION
Axinix 1 Tablet: Each film coated tablet contains Axitinib INN 1 mg.
Axinix 5 Tablet: Each film coated tablet contains Axitinib INN 5 mg.
CLINICAL PHARMACOLOGY
Mechanism of Action
Axitinib has been shown to inhibit receptor tyrosine kinases including
vascular endothelial growth
factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma
concentrations. These
receptors are implicated in pathologic angiogenesis, tumor growth, and
cancer progression.
VEGF-mediated endothelial cell proliferation and survival were
inhibited by Axitinib in vitro and in
mouse models. Axitinib was shown to inhibit tumor growth and
phosphorylation of VEGFR-2 in
tumor xenograft mouse models.
Pharmacodynamics
The effect of a single oral dose of Axitinib (5 mg) in the absence and
presence of 400 mg
Ketoconazole on the QTc interval was evaluated in a Randomized,
single-blinded, two-way
crossover study in 35 healthy subjects. No large changes in mean QTc
interval (i.e., >20 ms) from
placebo were detected up to 3 hours post-dose. However, small
increases in mean QTc interval
(i.e., <10 ms) cannot be ruled out.
Pharmacokinetics
The population pharmacokinetic analysis pooled data from 17 trials in
healthy subjects and
patients with cancer. A two-compartment disposition model with
first-order absorption and lag-time
adequately describes the Axitinib concentration-time profile.
Absorption and Distribution: Following single oral 5-mg dose
administration, the median
T
max
ranged from 2.5 to 4.1 hours. Based on the plasma half-life, steady
state is expected within 2
to 3 days of dosing. Dosing of Axitinib at 5 mg twice daily resulted
in approximately 1.4-fold
accumulation compared to administration of a single dose. At steady
state, Axitinib exhibits
approximately linear pharmacokinetics within the 1-mg to 20-mg dose
range. The mean absolute
bioavailability of Axitinib after an oral 5 mg dose is 58%.
Compared to overnight fasting, administration of Axitinib with a
moderate fat meal resulted in
10% lower AUC and a high fat, high-