Sunday, February 3, 2013

HERBIMYCIN AND AVASTIN

Based of the evidence presented on the Myristoylation story, we predict that the combination of dasatinib or Herbimycin  with Avastin will have a larger response  rate on Angiosarcoma and papillary cancers because of a combined suppression of VGEF and SRC/MEK.

Dasatinib

From Wikipedia, the free encyclopedia
Dasatinib
Systematic (IUPAC) name
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-
1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazole
carboxamide monohydrate
Clinical data
Trade names Sprycel












Pharmacokinetic data
Protein binding 96%
Metabolism Hepatic
Half-life 1.3 to 5 hours
Excretion Fecal (85%), renal (4%)


Yes
















Chemical data
Formula C22H26ClN7O2S 



Dasatinib, previously known as BMS-354825, is a cancer drug produced by Bristol-Myers Squibb and sold under the trade name Sprycel. Dasatinib is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML) after imatinib treatment and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). It is being evaluated for use in numerous other cancers, including advanced prostate cancer.
The drug is named after one of the inventor chemists, Jagabandhu Das, who was a member of the large discovery and development team at Bristol Myers Squibb.[1]

Herbimycin

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Herbimycin












Yes










Properties
Molecular formula C30H42N2O9
Molar mass 574.66 g/mol



Hazards







Herbimycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and alters its function. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, angiogenesis and oncogenesis.
It was originally found by its herbicidal activity, and thus named.

Synonyms

  • Antibiotic Tan 420F
  • Herbimycin A

Biological activity

Herbimycin induces the degradation of proteins that are mutated in tumor cells such as v-Src, Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90.

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Interferon  will have a reasonable role, and studies have certainly reported cases of response of Angiosarcoma to Interferon. At CRBCM and the GREATER East cancer Center we are following a case of a young 38 year old female who has been referred to us after receiving Gemzar and Taxotere followed by MAID x 3 cycles for a 12 cm Angiosarcoma in the liver.  She had an extensive skin reaction with desquamative feature to the Taxane.  We plan to start her on Avastin alone at this point. We understand Navelbine could have a role.
Her case will be presented at Tumor Board to completely exhaust salvage surgical resection option.  We are still awaiting a gene profiling which was not obtained at onset. An update will be forthcoming.
We are still working hard at CRBCM.
 Role of Nexavar has also been discussed in Angiosarcoma...

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