TFF Pharmaceuticals Announces Completion of Enrollment and Preliminary Data from its Phase 1 Clinical Trial of Tacrolimus Inhalation Powder
Inhaled Tacrolimus Powder Achieves Systemic Therapeutic Drug Levels
Anticipate Additional Safety Data in 3Q 2021
Initiation of Lung Transplant Study Expected in 2H 2021
As discussed during our recent Science Day event, lung transplant patients receiving tacrolimus for maintenance immunosuppression are carefully monitored so that drug concentration levels can be adjusted to achieve efficacious immunosuppression while minimizing toxicities. Following lung transplant, therapeutic drug monitoring (TDM) is used to achieve maintenance tacrolimus blood levels from 5-15 ng/mL to prevent acute allograft rejection.
In the Single Ascending Dose (SAD) phase of the trial, single doses of inhaled tacrolimus of 0.5 mg, 1.0 mg, 2.5 mg to 5.0 mg were administered to healthy subjects. Peak blood levels were measured 15 min after dosing, and trough blood levels were measured 12 hours after dosing for each subject. Peak levels were monitored to determine if they correlated with any acute adverse effects, while trough blood levels were measured to determine if subjects were reaching levels of tacrolimus that are sufficient for immunosuppression.
In the subjects that received inhaled tacrolimus in the low dose group, the mean trough blood levels reached 1.1 ng/mL, while blood levels in the highest dose group reached 10.0 ng/mL. In addition, when subjects received inhaled tacrolimus dosing at 2.5 mg while fasting or 30 minutes after a high fat meal, there were no significant differences in systemic exposure demonstrating that delivery by inhalation was not associated with food effects in this cohort of subjects. By contrast, the rate and extent of absorption of tacrolimus is significantly decreased when tacrolimus is administered orally when taken with food, and this effect is most pronounced after a high-fat meal.
Furthermore, during the Multiple Ascending Dose (MAD) phase, repeated dosing of inhaled tacrolimus every 12 hours over 7 days demonstrated that subjects receiving doses of 0.5 mg twice daily and 1.0 mg twice daily achieved 12-hour trough steady state blood levels that averaged 6.8 and 14.9 ng/mL, respectively. These data demonstrate that low dosing of Tacrolimus Inhalation Powder (0.5-1.0 mg) can achieve blood levels that are sufficient for efficacious immunosuppression.
“Completion of enrollment in the Phase 1 study of Tacrolimus Inhalation Powder represents a critical milestone for
In addition to leveraging its proprietary Thin Film Freezing technology platform to develop
About TFF Pharmaceuticals’ Thin Film Freezing technology platform
TFF Pharmaceuticals’ Thin Film Freezing (TFF) platform was designed to improve the solubility and absorption of poorly water-soluble drugs and is particularly suited to generate dry powder particles with properties targeted for inhalation delivery, especially to the deep lung, an area of extreme interest in respiratory medicine. The TFF process results in a “Brittle Matrix Particle,” which possesses low bulk density, high surface area, and typically an amorphous morphology, allowing the particles to supersaturate when contacting the target site, such as lung tissue. Based upon laboratory experiments the aerodynamic properties of the particles are such that the portion of a drug deposited to the deep lung has the potential to reach as high as 75 percent.
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Source: TFF Pharmaceuticals, Inc.