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Apamide (Apamide) is a second-generation nonsteroidal androgen receptor (AR) inhibitor, first developed by the University of California, USA, in 2009 authorized the Exclusive Development of Aragon Corporation, and in August 2013 Johnson and Johnson acquired Aragon, a subsidiary of Jansen Pharmaceuticals, which is responsible for the development, listing, production and sale of new drugs.
aparuamine has been approved for adaptation as non-metastatic derebelct-resistant prostate cancer (CRPC) and metastatic dealitatic-sensitive prostate cancer.
recently published in Clinical Cancer Research the results of clinical trials evaluating pharmacokinetics, safety, and anti-tumor activity in patients with aphrosemamines and aulated acetaminophen (AA-P) in metastatic CRPC patients.
the trial, a multi-centered, open-labeled Phase Ib drug interaction study, recruited 57 mCRPC patients, who were given 1000mg acetate a daily dose of 1000mg abitron ( 28 days of treatment) from the first day of the first course of treatment , and 240mg aparulamine (28 days a day) from C1D8.
collected blood samples at C1D7 and C2D8 for pharmacokinetic analysis.
when Aparuamine was used in conjunction with AA-P, the total exposure of Abitron, Pernison and Pernison was reduced by 14%, 61% and 42%, respectively. no increase in the adverse events associated with salt corticosteroid overdose saline
.
patients who had not been exposed to AR signal inhibitors had longer median treatment and had an even larger decline in prostate-specific antigens (PSA) compared to patients who had previously been treated.
in 80% (12/15) patients treated with AR signal inhibitors for initial use and 14% (6/42) of previous AR signal inhibitors, PSA was found to have decreased by more than 50% from baseline levels at any time. summary of
: Apaluamine combined with AA-P treatment of mCRPC patients (including patients progressing after treatment with AR signal inhibitors) was well tolerated and showed antitumor activity.
no significant pharmacokinetic interactions were observed between abitron and Aparuamines;
this study supports the treatment of mCRPC patients with this research protocol.
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