Lapatinib ditosylate
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Lapatinib ditosylate
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CAS No:
388082-77-7
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Formula:
C29H26ClFN4O4S.2C7H8O3S
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Chemical Name:
Lapatinib ditosylate
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Synonyms:
4-Quinazolinamine,N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-,4-methylbenzenesulfonate (1:2);4-Quinazolinamine,N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-,bis(4-methylbenzenesulfonate);Lapatinib ditosylate;GW 572016F;Tykerb
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CAS No:
Description
Yellow Solid
A quinazoline derivative that inhibits EPIDERMAL GROWTH FACTOR RECEPTOR and HER2 (RECEPTOR, ERBB-2) tyrosine kinases. It is used for the treatment of advanced or metastatic breast cancer, where tumors overexpress HER2.
Characteristics
240
12.32880
Yellow solid
240-2420C
750.7°C at 760 mmHg
407.8ºC
-20°C Freezer, Under Inert Atmosphere
Safety Information
24/25
P201, P202, P260, P263, P264, P270, P273, P281, P308+P313, P314, P405, P501
H360
Drug Information
Tyverb is indicated for the treatment of patients with breast cancer, whose tumours overexpress HER2 (ErbB2):in combination with capecitabine for patients with advanced or metastatic disease with progression following prior therapy, which must have included anthracyclines and taxanes and therapy with trastuzumab in the metastatic setting;in combination with trastuzumab for patients with hormone-receptor-negative metastatic disease that has progressed on prior trastuzumab therapy or therapies in combination with chemotherapy;in combination with an aromatase inhibitor for post-menopausal women with hormone-receptor-positive metastatic disease, not currently intended for chemotherapy. The patients in the registration study had not previously been treated with trastuzumab or an aromatase inhibitor. No data are available on the efficacy of this combination relative to trastuzumab in combination with an aromatase inhibitor in this patient population.|Drug: Lapatinibditosylate
Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)
GW 282974X
Lapatinib ditosylate Use and Manufacturing
Lapatinib Ditosylate (GW572016, GW2016, Tykerb, Tyverb) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
Human drugs -> Tyverb -> EMA Drug Category|Protein kinase inhibitors -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients
Computed Properties
Molecular Weight:753.3
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:12
Rotatable Bond Count:12
Exact Mass:752.1541476
Monoisotopic Mass:752.1541476
Topological Polar Surface Area:178
Heavy Atom Count:51
Complexity:1100
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes
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