Table 1. Drugs with evidence of affecting autophagy in ovarian cancer.
Most Frequent Adverse Events | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|
Drug | Target | Ref (PMID) | FDA approved? | Patent end date? | Autophagy stage | G1–2 | G3 | G4 | Safety Reference | Notes |
Nelfinavir | ER stress | 19106637 | Y | No patent | Initiation, compensation for ER stress | 17% | - | - | FDA (NDA 21–503) | |
Chloroquine | Lysosome | 19033662 | Y | No patent | Clearance | 2% | - | - | PMID 10759574 | |
Dasatinib | Src family | 20629079 | Y | 6/2020 | Initiation | 17% | 5% | FDA (NDA 21–986) | ||
Rapamycin | mTORC1 | 19033662 | Y | No patent | Initiation and expansion | 35% | 15% | 2% | PMID 21752435* | Temsirolimus |
Metformin | AMPK, LKB1 | 21532889 | Y | No patent | Stem cells or AMPK/LKB1/initiation | 8–13% | - | - | PMID 17638715 | |
Doxorubicin | DNA | 22860102 | Y | Equivalents | Initiation | 37% | 11% | FDA (NDA 50–718) | ||
Titanocene Y | DNA | 23019413 | N | - | Initiation | - | - | - | ||
Carboplatin | DNA | 21743489* | Y | No patent | Initiation, protective autophagy | 98% | FDA (NDA 20–452) | *cisplatin | ||
5-fluorouracil | DNA, ER stress | 22684338 | Y | Equivalents | Initiation | 33% | 52% | 42% | FDA (NDA 20–985) | |
Diindolylmethane | ER Stress | 22564965 | N* | - | Initiation | 0% | 0% | 0% | FDA (Docket 95s0316/sup0002) | *Supplement |
3-methyladenine | BECN1 | 24817946 | N | - | Initiation block, enhances cisplatin death | - | - | - | ||
Saquinavir | ER Stress | 19147209 | Y | 11/2015 | Initiation | 11% | - | - | FDA (NDA 21–785) | |
Fulvestrant | Estrogen receptor | 22896656 | Y | 1/2021 | Initiation | 68% | 10% | FDA (NDA 21–344) | ||
L-asparaginase | Glycosylation | 22333033 | Y | No patent | Initiation | 28% | 5% | FDA (125359 Orig1s000) | ||
Suberoylanilide hydroxamic acid | HDAC | 21491416 | Y | 2/2025 | Initiation | 58% | 4% | FDA (NDA 21–991) | ||
Bafilomycin | Lysosome | 22564965 | N | - | Clearance | - | - | - | ||
SB202190 | MAPK | 21853067 | N | - | Clearance | - | - | - | ||
Decitabine | Methylcytosine | 21491416 | Y | Equivalents | Initiation | - | 27% | 93% | 16532500 and FDA (NDA 205582) | |
Paclitaxel | Microtubules | 22430212 | Y | Equivalents | Initiation | - | 46% | FDA (NDA 20–262/S-024) | ||
Wortmannin | PI3K | 21853067 | N | - | Initiation | (toxic) | PMID 2527336 | |||
Bortezomib | Proteasome | 19584239 | Y | 10/2014 | Proteasome disruption | 100% | 61% | 14% | FDA (NDA 21–602) | |
MG132 | Proteasome | 23270461 | N | - | Proteasome disruption | - | - | - | ||
H2O2 | ROS | 23047606 | N | - | Initiation | - | - | - | ||
FTY720 | S1P receptor | 20935520 | Y | 2/2019 | Initiation, siBECN1 and siLC3 block effect | 9% | - | - | FDA (NDA 22–527) | |
Arsenic trioxide | Unknown | 22919067 | Y | 11/2018 | Initiation (less pAkt) | 75% | 13% | FDA (NDA 21–248) | ||
Withafarin A | Vimentin | 22860102 | N | - | Initiation | - | - | - |