Novel hormonal therapies in the management of advanced prostate cancer: extrapolating Asian findings to Southeast Asia

Table 1 Molecular differences between the new-generation ARATs

	Abiraterone acetate	Enzalutamide	Apalutamide	Darolutamide
Molecular structure [54,55,56,57]
Ability to cross the blood–brain barrier [19, 34]	Yes
AR inhibition (AR-HEK293 cells) [34]	n.a.	Full antagonist (IC₅₀ = 219 nM)	Full antagonist (IC₅₀ = 200 nM)	Full antagonist (IC₅₀ = 26 nM)
Molecular weight [54,55,56,57]	391.5	464.44	477.4	398.8
pK_a of molecule [57,58,59,60]	5.19	No pK_a between pH 3–11	9.7	11.75
Computed LogP [54,55,56,57]	5.2	3.6	3	1.8
Activation of mutant AR [34]	n.a.	Yes (7877L)	Yes (7877L)	None described
Packing size [60,61,62,63]	250 mg and 500 mg tablets	40 mg capsules	60 mg tablets	300 mg tablets
Recommended dosage [60,61,62,63]	1000 mg/day	160 mg/day	240 mg/day	1200 mg/day
Availability in SEA countries (as of January 2022)	Malaysia, Singapore, Indonesia, Thailand, Philippines, Vietnam	Malaysia, Singapore, Indonesia, Thailand, Philippines	Malaysia, Singapore, Indonesia, Thailand	Singapore

AR androgen receptor, BD twice daily, IC₅₀ half maximal inhibitory concentration, n.a. not applicable, OD once daily, SEA Southeast Asia

ISSN: 1471-2490