. 2022 Jan 21;10(1):e003766. doi: 10.1136/jitc-2021-003766

Table 1.

In vitro effective doses of ruxolitinib, sirolimus, everolimus, temsirolimus and dasatinib as well as their respective clinical dose(s) and corresponding exposure(s)

Kinase inhibitor	Target	In vitro effective dose (nM)	In vitro effective dose (ng/mL)	Clinical dose	Clinical exposure	References
Ruxolitinib	JAK1/2	50–100	15.3–30.6	5 mg/day (oral)	C_max=195 (35.4) ng/mL* t_1/2=2.6 (40) hours*	NDA 202109250
				10 mg/day (oral)	C_max=368 (29.9) ng/mL* t_1/2=3.4 (41) hours*
				25 mg/day (oral)	C_max=934 (55.9) ng/mL* t_1/2=3.0 (22) hours*
Sirolimus	mTOR	10–100	9.1–91.4	2 mg/day (oral)	C_max=12.2 +/− 6.2 ng/mL t_max=3.01+/− 2.4 hours	NDA 21–083/S-034 NDA 21–110/S-045
Sirolimus	mTOR	10–100	9.1–91.4	5 mg/day (oral)	C_max=37.4 +/− 21 ng/mL t_max=1.84 +/− 1.3 hours	NDA 21–083/S-034 NDA 21–110/S-045
Everolimus	mTOR	10–100	9.6–95.8	5 mg/day (oral)	C_max=28.7 ng/ mL* t_1/2=31.2 (4.79) hours†	NDA 21–56047
Temsirolimus	mTOR	10–100	10.3–103.0	25 mg/week (intravenously)	C_max=585 (83) ng/mL† t_1/2=17.3 (5.9) hours†	NDA 22–08851
Dasatinib	Src/lck	50–100	24.4–48.8	100 mg/day (oral)	C_max=54.6 ng/mL* (56) t_max=1.00, (0.5, 4.00) hours‡	NDA 21–986 NDA 22–07252

*Geometric mean (per cent coefficient of variation (%)).

†Mean (SD).

‡Median (min, max).