Примери за използване на Tipiracil на Английски и техните преводи на Български
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Contribution of tipiracil hydrochloride.
The active substances are trifluridine and tipiracil.
Plasma protein binding of tipiracil hydrochloride was below 8%.
Each tablet contains 15 mg trifluridine and 6.14 mg tipiracil.
Tipiracil increases the level of trifluridine in the blood by slowing its breakdown.
Хората също превеждат
Lonsurf contains two different active substances:trifluridine and tipiracil.
Twelve-month OS rates were 21.2% in the trifluridine/tipiracil group and 13.0% in the placebo group.
NAME OF THE MEDICINAL PRODUCT Lonsurf 20 mg/8.19 mg film-coated tablets trifluridine/tipiracil.
Tipiracil stops the trifluridine from being broken down by the body, helping trifluridine to work longer.
Each film-coated tablet contains 20 mg trifluridine and 8.19 mg tipiracil(as hydrochloride).
The mean t1/2 values for tipiracil hydrochloride on Day 1 of Cycle 1 and on Day 12 of Cycle 1 were 2.1 hours and 2.4 hours, respectively.
Results of animal studies did not indicate an effect of trifluridine and tipiracil hydrochloride on male and female fertility in rats.
Transport of tipiracil hydrochloride by OCT2 and MATE1 might be affected when Lonsurf is administered concomitantly with inhibitors of OCT2 and MATE1.
As for the other exposure parameters of trifluridine and tipiracil hydrochloride, those appeared to be dose proportional.
The PK of trifluridine and tipiracil hydrochloride have not been studied in patients with severe renal impairment or end-stage renal disease(see section 4.4).
We will continue to collaborate with regulatory bodies to progress our mission to make trifluridine/tipiracil accessible to patients and medical professionals.".
Thus trifluridine and tipiracil hydrochloride are not expected to cause or be subject to a significant medicinal product interaction mediated by CYP.
Based on the population PK analysis, there is no clinically relevant effect of age, gender orrace on the PK of trifluridine or tipiracil hydrochloride.
Studies in animals have shown excretion of trifluridine, tipiracil hydrochloride and/or their metabolites in milk(see section 5.3).
Tipiracil hydrochloride was a substrate for OCT2 and MATE1, therefore, the concentration might be increased when Lonsurf is administered concomitantly with inhibitors of OCT2 or MATE1.
In vitro evaluation indicated that trifluridine, tipiracil hydrochloride and FTY had no inductive effect on human CYP1A2, CYP2B6 or CYP3A4/5.
Following a single dose of Lonsurf(35 mg/m2) in patients with advanced solid tumours, the apparent volume of distribution(Vd/F)for trifluridine and tipiracil hydrochloride was 21 L and 333 L, respectively.
In vitro evaluation indicated that trifluridine, tipiracil hydrochloride and FTY had no inductive effect on human CYP isoforms(see section 5.2).
Lonsurf is comprised of an antineoplastic thymidine-based nucleoside analogue, trifluridine, andthe thymidine phosphorylase(TPase) inhibitor, tipiracil hydrochloride, at a molar ratio 1:0.5 weight ratio.
In vitro studies indicated that trifluridine, tipiracil hydrochloride and 5-[trifluoromethyl] uracil(FTY) did not inhibit the activity of human cytochrome P450(CYP) isoforms.
Following a single dose of Lonsurf(35 mg/m2) in patients with advanced solid tumours, the mean times to peak plasma concentrations(tmax)of trifluridine and tipiracil hydrochloride were around 2 hours and 3 hours, respectively.
Neither trifluridine nor tipiracil hydrochloride was an inhibitor of or substrate for human uptake and efflux transporters based on in vitro studies, except for OCT2 and MATE1.
Half-life time(t1/2) andthe accumulation ratio of trifluridine and tipiracil hydrochloride were similar between the moderate, mild and normal hepatic function patients.
In vitro studies indicated that trifluridine, tipiracil hydrochloride and FTY(inactive metabolite of trifluridine) did not inhibit the CYP isoforms tested(CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4/5).
However, there was no accumulation for tipiracil hydrochloride, and no further accumulation of trifluridine with successive cycles(Day 12 of Cycles 2 and 3) of administration of Lonsurf.