Afinitor

Država: Avstralija

Jezik: angleščina

Source: Department of Health (Therapeutic Goods Administration)

Aktivna sestavina:

Everolimus

Dostopno od:

Novartis Pharmaceuticals Australia Pty Ltd

Razred:

Medicine Registered

Navodilo za uporabo

AFINITOR
®

_everolimus_
CONSUMER MEDICINE INFORMATION

WHAT IS IN THIS LEAFLET
This leaflet answers some common
questions about Afinitor.
It does not contain all the available
information. It does not take the
place of talking to your doctor or
pharmacist.
The information in this leaflet was
last updated on the date listed on the
final page. More recent information
on the medicine may be available.
YOU SHOULD ENSURE THAT YOU SPEAK
TO YOUR PHARMACIST OR DOCTOR TO
OBTAIN THE MOST UP TO DATE
INFORMATION ON THE MEDICINE. YOU
CAN ALSO DOWNLOAD THE MOST UP TO
DATE LEAFLET FROM
WWW.NOVARTIS.COM.AU.
Those updates may contain important
information about the medicine and
its use of which you should be aware.
All medicines have risks and
benefits. Your doctor has weighed
the risks of you taking Afinitor
against the benefits they expect it
will have for you.
IF YOU HAVE ANY CONCERNS ABOUT
TAKING THIS MEDICINE, ASK YOUR
DOCTOR OR PHARMACIST.
KEEP THIS LEAFLET WITH THE MEDICINE.
You may need to read it again.
WHAT AFINITOR IS USED
FOR
Afinitor is used in the treatment of
renal cell carcinoma, a type of kidney
cancer; pancreatic neuroendocrine
tumours (pNET), a type of cancer
located in the pancreas; tuberous
sclerosis complex (TSC) with
angiomyolipoma of the kidney (a
kidney tumour) not requiring
immediate surgery; or TSC with
subependymal giant cell astrocytoma
(sometimes called 'SEGA'), a specific
type of brain tumour not requiring
immediate surgery.
Afinitor is also used in the treatment
of hormone receptor-positive HER2
negative advanced breast cancer in
postmenopausal women, in
conjunction with exemestane after
failure of letrozole or anastrozole.
It is only used in patients whose
tumour has tested negative to HER2.
Everolimus is the active substance in
Afinitor.
TREATMENT OF KIDNEY CANCER
Afinitor stops the cancer from
making new cells and cuts off the
blood supply. This slows the growth
and spread of the cancer.
TREATMENT OF PNET
Afinitor is used to control the growth
of these tumours located in the
panc

Lastnosti izdelka

Page 1 of 46 
AFINITOR
®

(EVEROLIMUS) 
NAME OF THE MEDICINE 

The active ingredient of Afinitor 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: 

N
O
O
O
O
O
O
O
OH
O
O
O
OH
OH
O

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: (Tablets) Butylated
hydroxytoluene, magnesium stearate, lactose monohydrate, 
hypromellose, crospovidone, lactose anhydrous. 

Page 2 of 46 
Excipients: (dispersible tablets) Butylated hydroxytoluene,
magnesium stearate, lactose 
monohydrate, hypromellose, crospovidone, mannitol,
cellulose microcrystalline, and silica 
colloidal anhydrous. 

PHARMACOLOGY 
PHARMACODYNAMICS 
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