TEVA-EVEROLIMUS everolimus 7.5 mg tablet blister pack

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

everolimus, Quantity: 7.5 mg

Available from:

Medis Pharma Pty Ltd

INN (International Name):

Everolimus

Pharmaceutical form:

Tablet

Composition:

Excipient Ingredients: butylated hydroxytoluene; hypromellose; lactose monohydrate; lactose; crospovidone; magnesium stearate

Administration route:

Oral

Units in package:

10 tablets, 30 tablets, 50 tablets, 60 tablets, 90 tablets

Prescription type:

(S4) Prescription Only Medicine

Therapeutic indications:

The treatment of: - Postmenopausal women with hormone receptor-positive, HER2 negative advanced breast cancer in combination with exemestane after failure of treatment with letrozole and anastrozole - Progressive, unresectable or metastatic, well or moderately differentiated neuroendocrine tumours (NETs) of pancreatic origin - Advanced renal cell carcinoma after failure of treatment with sorafenib or sunitinib - Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC) who require therapeutic intervention but are not candidates for curative surgical resection - Patients with tuberous sclerosis complex (TSC) who have renal angiomyolipoma not requiring immediate surgery.

Product summary:

Visual Identification: White, oblong, flat, bevelled edge tablets, marked with "EV" on one side and "7.5" on the other; Container Type: Blister Pack; Container Material: PA/Al/PVC/Al - polyamide-aluminium foil-polyvinylchloride/aluminium foil; Container Life Time: 2 Years; Container Temperature: Store below 25 degrees Celsius

Authorization status:

Licence status A

Authorization date:

2017-04-20

Summary of Product characteristics

Product Information
Page 1
TEVA-EVEROLIMUS 2.5 mg, 5 mg, 7.5 mg & 10 mg Tablets
TEVA-EVEROLIMUS
(EVEROLIMUS)
NAME OF THE MEDICINE
The active ingredient of Teva-Everolimus is everolimus.
The chemical name is 40-O-(2-hydroxyethyl)-rapamycin or
40-O-(2-hydroxyethyl)-sirolimus.
Its molecular formula is C
53
H
83
NO
14
and its molecular weight is 958.2.
The structural formula of everolimus is:
DESCRIPTION
Everolimus is a white to faintly yellow powder practically insoluble
in water but soluble in
organic solvents such as ethanol and methanol.
CAS number: 159351-69-6
Excipients: Butylated hydroxytoluene, magnesium stearate, lactose
monohydrate, hypromellose,
crospovidone, lactose.
Teva Pharma Australia Pty Ltd
Version 1.0
2017-04-21
Product Information
Page 2
TEVA-EVEROLIMUS 2.5 mg, 5 mg, 7.5 mg & 10 mg Tablets
PHARMACOLOGY
PHARMACODYNAMIC
s
MECHANISM OF ACTION
Everolimus is a signal transduction inhibitor targeting mTOR
(mammalian target of rapamycin),
or more specifically, mTORC1 (mammalian 'target of rapamycin' complex
1). mTOR is a key
serine-threonine kinase playing a central role in the regulation of
cell growth, proliferation and
survival. The regulation of mTORC1 signalling is complex, being
modulated by mitogens, growth
factors, energy and nutrient availability. mTORC1 is an essential
regulator of global protein
synthesis downstream on the PI3K/AKT pathway, which is dysregulated in
the majority of human
cancers.
Constitutive activation of the PI3K/Akt/mTOR pathway can contribute to
endocrine resistance in
breast cancer.
_In vitro _
studies show that oestrogen-dependent and HER2+ breast cancer cells
are
sensitive to the inhibitory effects of everolimus, and that
combination of everolimus with Akt,
HER2, or aromatase inhibitors synergistically enhances the anti-tumour
effect of everolimus.
Two primary regulators of mTORC1 signaling are the oncogene
suppressors tuberin-sclerosis
complexes 1 & 2 (TSC1, TSC2). Loss or inactivation of either TSC1 or
TSC2 leads to elevated
rheb-GTP levels, a ras family GTPase, which