Product information and disease description Product description Product information Pharmacology

Pharmacokinetics

6 evidence topics · 4 sources

In vitro release: sponsor description of three-year release

“Additionally, long-term in vitro release studies have demonstrated that our BIM-IOL System delivered bimatoprost in a sustained and consistent manner over multiple years.” (opens the source at this quote in a new tab)
“Consistent Daily Release of Bimatoprost in vitro Maintained Over Three Years” (opens the source at this quote in a new tab)

Pad elution data: in vitro release rate and aqueous humor concentrations in dogs

“As illustrated in FIG. 8 , which is a graph 800 of daily release or elution (in micrograms) of Bimatoprost in vitro versus time (day), the release rate over a four-hundred-day study is essentially a zero-order and/or a steady state elution rate. The target release rate in this study on rabbits was 0.050 to 0.100 micrograms per day. As illustrated in FIG. 8 , the average release rate is slightly less than 0.100 micrograms per day with a range of about 0.075 micrograms to about 0.100 micrograms.” (opens the source at this quote in a new tab)
“As found with the low dose group (Grp 1), the mid-dose group (Grp 2), and the high dose group (Grp 3), the level of Bimatoprost in the aqueous humor exhibited a zero-order elution rate over the study period of about one hundred thirteen days.” (opens the source at this quote in a new tab)

Pad configurations and target daily release rates described in patent filings

“In certain embodiments, the drug delivery system 700 of FIG. 7A is sized and configured for about a three-year release of the therapeutic agent, with a release rate of about 80 to about 150 nanograms (ng) per day (e.g., about 120 ng/day bimatoprost). By decreasing the surface area of the drug delivery component 80, as illustrated in FIG. 7B, the drug delivery system 700 is sized and configured for about a three-year release of the at least one therapeutic agent with a release rate of about 60 ng per day, (e.g., bimatoprost).” (opens the source at this quote in a new tab)

Systemic exposure: nonclinical toxicokinetics

“Following bilateral administration, plasma levels of the bimatoprost and bimatoprost acid remained below the lower limit of quantitation for all samples collected at all time points, indicating no systemic exposure.” (opens the source at this quote in a new tab)

Bimatoprost absorption, distribution, metabolism, and excretion: Lumigan labeling

“Bimatoprost is moderately distributed into body tissues with a steady-state volume of distribution of 0.67 L/kg. In human blood, bimatoprost resides mainly in the plasma. Approximately 12% of bimatoprost remains unbound in human plasma.” (opens the source at this quote in a new tab)
“Bimatoprost is the major circulating species in the blood once it reaches the systemic circulation following ocular dosing. Bimatoprost then undergoes oxidation, N-deethylation and glucuronidation to form a diverse variety of metabolites.” (opens the source at this quote in a new tab)
“Following an intravenous dose of radiolabeled bimatoprost (3.12 mcg/kg) to six healthy subjects, the maximum blood concentration of unchanged drug was 12.2 ng/mL and decreased rapidly with an elimination half-life of approximately 45 minutes. The total blood clearance of bimatoprost was 1.5 L/hr/kg. Up to 67% of the administered dose was excreted in the urine while 25% of the dose was recovered in the feces.” (opens the source at this quote in a new tab)

Systemic exposure after intracameral bimatoprost: Durysta labeling

“After a single administration of DURYSTA, bimatoprost concentrations were below the lower limit of quantitation (0.001 ng/mL) in the majority (approximately 92%) of patients. The maximum bimatoprost concentration observed in any patient was 0.00224 ng/mL.” (opens the source at this quote in a new tab)

Human aqueous humor or plasma pharmacokinetics of the BIM-IOL System

No evidence found.