TABLE 1.

Examples of FDA-approved drugs that could downregulate ABCB1/ABCG2 and provide a window-in-time for brain drug delivery

Target	Drug Name	Drug Action	Predicted Outcome
COX-2	Fenoprofen	Inhibitor	ABCB1 ↓
COX-2	Acetic salicylic acid	Inhibitor	ABCB1 ↓
COX-2	Diclofenac	Inhibitor	ABCB1 ↓
COX-2	Celecoxib	Inhibitor	ABCB1 ↓
COX-2	Bromfenac	Inhibitor	ABCB1 ↓
COX-2	Etoricoxib	Inhibitor	ABCB1 ↓
COX-2	Firocoxib	Inhibitor	ABCB1 ↓
COX-2	Flurbiprofen	Inhibitor	ABCB1 ↓
COX-2	Ibuprofen	Inhibitor	ABCB1 ↓
COX-2	Indomethacin	Inhibitor	ABCB1 ↓
COX-2	Ketorolac	Inhibitor	ABCB1 ↓
COX-2	Meloxicam	Inhibitor	ABCB1 ↓
COX-2	Nabumetone	Inhibitor	ABCB1 ↓
COX-2	Naproxen	Inhibitor	ABCB1 ↓
COX-2	Oxaprozin	Inhibitor	ABCB1 ↓
COX-2	Parecoxib	Inhibitor	ABCB1 ↓
COX-2	Piroxicam	Inhibitor	ABCB1 ↓
COX-2	Tenoxicam	Inhibitor	ABCB1 ↓
EGFR	Cetuximab	EGFR neutralizing antibody	ABCB1 ↓; ABCG2 ↓
EGFR	Erlotinib	Inhibitor	ABCB1 ↓; ABCG2 ↓
EGFR	Lapatinib	Inhibitor	ABCB1 ↓; ABCG2 ↓
EGFR	Mobocertinib	Inhibitor	ABCB1 ↓; ABCG2 ↓
EGFR	Necitumumab	EGFR neutralizing antibody	ABCB1 ↓; ABCG2 ↓
EGFR	Osimertinib	Inhibitor	ABCB1 ↓; ABCG2 ↓
EGFR	Panitumumab	EGFR neutralizing antibody	ABCB1 ↓; ABCG2 ↓
EGFR	Gefitinib	Inhibitor	ABCB1 ↓; ABCG2 ↓
ER	Estradiol	Agonist	ABCB1 ↓; ABCG2 ↓
ER	Estramustine	Agonist	ABCB1 ↓; ABCG2 ↓
ER	Ethinyl estradiol	Agonist	ABCB1 ↓; ABCG2 ↓
ER	Norethisterone	Agonist	ABCB1 ↓; ABCG2 ↓
ER	Norethynodrel	Agonist	ABCB1 ↓; ABCG2 ↓
GR	Mifepristone	Antagonist	ABCB1 ↓; ABCG2 ↓
GR	Ulipristal	Antagonist	ABCB1 ↓; ABCG2 ↓
MR	Fineronone	Antagonist	ABCB1 ↓; ABCG2 ↓
NMDAR	Esketamine	Antagonist	ABCB1 ↓
NMDAR	Memantine	Antagonist	ABCB1 ↓
mTOR	Everolimus	Inhibitor	ABCB1 ↓; ABCG2 ↓
mTOR	Sirolimus	Inhibitor	ABCB1 ↓; ABCG2 ↓
mTOR	Temsirolimus	Inhibitor	ABCB1 ↓; ABCG2 ↓
PI3K	Alpelisib	Inhibitor	ABCB1 ↓; ABCG2 ↓
PI3K	Copanlisib	Inhibitor	ABCB1 ↓; ABCG2 ↓
PI3K	Duvelisib	Inhibitor	ABCB1 ↓; ABCG2 ↓
TNFα	Adalimumab	TNFα neutralizing antibody	ABCB1 ↓
TNFα	Certolizumab	TNFα neutralizing antibody	ABCB1 ↓
TNFα	Etanercept	TNFα inhibitor	ABCB1 ↓
TNFα	Golimumab	TNFα neutralizing antibody	ABCB1 ↓
TNFα	Infliximab	TNFα neutralizing antibody	ABCB1 ↓

Materials and FDA-approval status were determined based on the FDALabel database in September 2021 (https://www.fda.gov/science-research/bioinformatics-tools/fdalabel-full-text-search-drug-product-labeling), specifically Section 12.1, “Mechanism of Action.”