Larotrectinib Sulfate
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Larotrectinib Sulfate
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CAS No:
1223405-08-0
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Formula:
C21H24F2N6O6S
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Chemical Name:
Larotrectinib Sulfate
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Synonyms:
LOXO-101 (sulfate);Larotrectinib/LOXO 101/ARRY 470 sulfate;ARRY 470) sulfate;Larotrectinib sulfate;Larotrectinib(LOXO 101;Larotrectinib (LOXO-101) sulfate;1-Pyrrolidinecarboxamide, N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-, (3S)-, sulfate (1:1);ARRY-470, Larotrectinib
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CAS No:
Description
Larotrectinib (LOXO-101) sulfate is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
Larotrectinib Sulfate is the sulfate salt form of larotrectinib, an orally available, tropomyosin receptor kinase (Trk) inhibitor, with potential antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.
Larotrectinib Sulfate Basic Attributes
526.52
526.144592
232-655-5
RDF76R62ID
C156895
Light yellow to brown
L01XE53
Drug Information
Vitrakvi as monotherapy is indicated for the treatment of adult and paediatric patients with solid tumours that display a Neurotrophic Tyrosine Receptor Kinase (NTRK) gene fusion,who have a disease that is locally advanced, metastatic or where surgical resection is likely to result in severe morbidity, andwho have no satisfactory treatment options.
Larotrectinib Sulfate Use and Manufacturing
Larotrectinib Sulfate is a potent and selective oral ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
Human drugs -> Vitrakvi -> EMA Drug Category|Antineoplastic agents -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients
Computed Properties
Molecular Weight:526.5
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:11
Rotatable Bond Count:3
Exact Mass:526.14461000
Monoisotopic Mass:526.14461000
Topological Polar Surface Area:169
Heavy Atom Count:36
Complexity:741
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes
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