Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as tofacitinib modified release (MR), tofacitinib modified-release (MR) formulation, tofacitinib modified-release formulation
tofacitinib modified release · 3 trials · 1 indication
Area Under the Curve From Time Zero to Extrapolated Infinite Time \[AUC (0 - ∞)\]
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) of Modified Release (MR) formulation compared to Immediate Release (IR) solution
Maximum (or peak) plasma concentration of MR formulation compared to IR solution
Maximum time to peak plasma concentration of MR formulation compared to IR solution
| Arm | Type | Description |
|---|---|---|
| Treatment A | EXPERIMENTAL | Single oral 10 mg dose of tofacitinib MR E1 administered in the fasted state. |
| Treatment B | EXPERIMENTAL | Single oral 10 mg dose of tofacitinib MR E2 administered in the fasted state. |
| Treatment C | EXPERIMENTAL | Single oral 10 mg dose of tofacitinib MR E3 administered in the fasted state. |
| Treatment D | EXPERIMENTAL | Single oral 10 mg dose of tofacitinib MR E1 administered in the fed state. |
| Treatment E | EXPERIMENTAL | Single oral 10 mg dose of tofacitinib MR E3 administered in the fed state. |
| Treatment F | ACTIVE_COMPARATOR | Single oral 10 mg dose of tofacitinib IR Solution (10 mL of the 1 mg/mL solution) administered in the fasted state. |
| tofacitinib MR 11 mg Fed | EXPERIMENTAL | tofacitinib modified release (MR) 11 mg tablet administered with food. |
| tofacitinib MR 11 mg Fasting | EXPERIMENTAL | tofacitinib modified release (MR) 11 mg tablet administered without food. |
| Experimental Treatment A | EXPERIMENTAL | A single dose of 11 mg tofacitinib modified-release (MR) administered in a fasting state. |
| Experimental Treatment B | EXPERIMENTAL | A single dose of 22 mg tofacitinib modified-release (MR) administered in a fasting state. |
| Name | Type | Description |
|---|---|---|
| tofacitinib modified release (MR) | DRUG | Single oral 10 mg multi particulate dose of dose of tofacitinib MR with different levels of enteric coating (MR E1, MR E2, and MR E3) in the fasted state. Additionally, the lowest and highest enteric coating levels will also be evaluated in the fed state. Treatment F: a 10 mg oral dose of tofacitinib IR solution |
| tofacitinib modified-release (MR) formulation | DRUG | A single dose of tofacitinib modified release 11 mg tablet after receiving the standard FDA high fat/high calorie meal. |
Inclusion Criteria: * Healthy male and/or female subjects of non-childbearing potential between the ages of 18 and 55 years, inclusive. * Female subjects of non-childbearing potential must meet at least 1 of the following criteria: 1. . Achieved postmenopausal status, defined as: cessation of re...
Tofacitinib modified release is an extended or modified-release oral tablet formulation of tofacitinib, a small molecule JAK inhibitor developed by Pfizer. It is designed to release the drug in a controlled manner rather than as an immediate-release dose. The formulation has been studied in Phase 1 clinical trials in healthy volunteers.
Tofacitinib modified release targets the Janus kinase family, specifically JAK3, JAK1, JAK2, and TYK2. It acts as an inhibitor of these kinases. By inhibiting JAK enzymes, the drug interferes with cytokine signaling pathways involved in immune and inflammatory responses.
Tofacitinib modified release is developed by Pfizer, Inc., which trades on the New York Stock Exchange under the ticker PFE. Pfizer is the sponsor of the Phase 1 clinical trials evaluating this modified-release formulation of tofacitinib.
Tofacitinib modified release is in Phase 1 clinical development. All three of its recorded trials are Phase 1 studies, and all three have been completed. The formulation is investigational and has not been approved by the FDA as a modified-release product.
Three completed Phase 1 trials have evaluated tofacitinib modified release: NCT04338711, which studied once-daily dosing of age-appropriate modified-release formulations in healthy adults; NCT02084875, which assessed the effect of food on 11 milligram modified-release tablets; and NCT01731327, which evaluated pharmacokinetics, safety, and bioavailability.
Yes. Tofacitinib modified release is also known as tofacitinib modified release (MR), tofacitinib modified-release (MR) formulation, and tofacitinib modified-release formulation. These names all refer to the same modified-release oral tablet version of tofacitinib developed by Pfizer.