Tykerb tablet 250mg

Country: Singapore

Language: English

Source: HSA (Health Sciences Authority)

Active ingredient:

Lapatinib Ditosylate 405.0mg eqv Lapatinib

Available from:

NOVARTIS (SINGAPORE) PTE LTD

ATC code:

L01XE07

Dosage:

250.00mg

Pharmaceutical form:

TABLET, FILM COATED

Composition:

Lapatinib Ditosylate 405.0mg eqv Lapatinib 250.00mg

Administration route:

ORAL

Prescription type:

Prescription Only

Manufactured by:

Glaxo Operations UK Ltd (trading as GlaxoWellcome Operations)

Authorization status:

ACTIVE

Authorization date:

2007-10-25

Patient Information leaflet

- 1 of 26-      
TYKERB™  
(LAPATINIB DITOSYLATE) 
250 MG TABLETS 

NAME OF THE DRUG 

TYKERB film-coated tablets contain lapatinib ditosylate which is a
member of 4-
anilinoquinazoline class of kinase inhibitors.  The chemical name for (IUPAC) 
lapatinib ditosylate is N-(3-chloro-4-{[(3-fluorophenyl) methyl]oxy}phenyl)-6-[5-
({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine bis(4-
methylbenzenesulfonate) monohydrate. 

The structural formula is: 

Molecular formula: C
29
H
26
ClFN
4
O
4
S(C
7
H
8
O
3
S)
2
H
2
O 
Molecular weight: 943.48 (ditosylate monohydrate) 
CAS number: 388082-78-8 

DESCRIPTION 
Lapatinib ditosylate monohydrate is a yellow solid, and
its solubility in water is 0.007 
mg/mL and in 0.1N HCl is 0.001 mg/mL at 25 
°C. 

TYKERB 250 mg film-coated tablets contain
microcrystalline cellulose, povidone 
K30, sodium starch glycolate, magnesium stearate, hypromellose,
titanium dioxide, 
macrogol 400, Polysorbate 80, Iron oxide red (CI77491) and Iron
oxide yellow 
(CI77492). 

PHARMACOLOGY 

PHARMACODYNAMICS 

- 2 of 26-      
ATC Code: 
L01XE07 

Lapatinib is a potent, reversible, and selective inhibitor of the intracellular tyrosine 
kinase domains of both ErbB1
(EGFR) and HER2 (ErbB2) receptors (estimated Ki
app

values of 3nM and 13nM, respectively) with a slow off-rate
from these receptors 
(half-life greater than or equal to 300 minutes).
This dissociation rate from ErbB1  
was found to be slower for lapatinib than for erlotinib and
gefitinib. Lapatinib inhibits 
tumour cell proliferation _in vitro_, and inhibits the growth
of ErbB1 (EGFR) and HER2 
over-expressing xenograft tumours in mice. Inhibition
of tumour growth was 
associated with decreased phosphorylation of ErbB1 (EGFR) and HER2
in tumour 
tissue. 

The growth inhibitory effects of lapatinib we

Summary of Product characteristics

Tykerb Aug 2021.SIN
Page 1 of 28
TYKERB™
(LAPATINIB DITOSYLATE)
250 MG FILM COATED TABLETS
TRADENAME
Tykerb
TM
Film-coated tablets 250 mg lapatinib
DESCRIPTION AND COMPOSITION
TYKERB film-coated tablets contain lapatinib ditosylate which is a
member of 4-
anilinoquinazoline class of kinase inhibitors. The chemical name for
(IUPAC) lapatinib
ditosylate is N-(3-chloro-4-{[(3-fluorophenyl)
methyl]oxy}phenyl)-6-[5- ({[2-
(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine
bis(4-
methylbenzenesulfonate) monohydrate. lapatinib
Lapatinib ditosylate monohydrate is a yellow solid, and its solubility
in water is 0.007
mg/mL and in 0.1N HCl is 0.001 mg/mL at 25°C
EXCIPIENTS
YELLOW FILM-COATED TABLETS
Microcrystalline cellulose
Povidone K30
Sodium starch glycolate (Type A)
Magnesium stearate
Hypromellose
Titanium dioxide
Macrogol 400
Polysorbate 80
Iron oxide red (C177491)
Iron oxide yellow (C177492)
Tykerb Aug 2021.SIN
Page 2 of 28
CLINICAL PHARMACOLOGY
PHARMACOTHERAPEUTIC GROUP, ATC
Human epidermal growth factor receptor 2 (HER)2 tyrosine kinase
inhibitor, L01EH01.
MECHANISM OF ACTION (MOA)
Tykerb is a potent, reversible, and selective inhibitor of the
intracellular tyrosine kinase
domains of both ErbB1 (EGFR) and HER2 (ErbB2) receptors (estimated
Kiapp values of
3nM and 13nM, respectively) with a slow off-rate from these receptors
(half-life ≥ 300
minutes). This dissociation rate from ErbB1 was found to be slower for
Tykerb than for
erlotinib and gefitinib. Tykerb inhibits tumour cell proliferation in
vitro, and inhibits the
growth of ErbB1 (EGFR) and HER2 over-expressing xenograft tumours in
mice.
Inhibition of tumour growth was associated with decreased
phosphorylation of ErbB1
(EGFR) and HER2 in tumour tissue.
The growth inhibitory effects of Tykerb were evaluated in
trastuzumab-conditioned cell
lines. Tykerb retained significant activity against breast cancer cell
lines selected for
resistance to trastuzumab by long-term growth in
trastuzumab-containing medium
_in _
_vitro_
. These findings suggest n