Investigational Drug Details
| Drug ID: | D396 |
| Drug Name: | Hydroxychloroquine |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB01611 |
| DrugBank Description: | Hydroxychloroquine is a racemic mixture consisting of an R and S enantiomer.[A183047] Hydroxychloroquine is an aminoquinoline like [chloroquine].[L8072] It is a commonly prescribed medication in the treatment of uncomplicated malaria, rheumatoid arthritis, chronic discoid lupus erythematosus, and systemic lupus erythematosus.[L8072] Hydroxychloroquine is also used for the prophylaxis of malaria in regions where chloroquine resistance is unlikely.[L8072] Hydroxychloroquine was developed during World War II as a derivative of [quinacrine] with less severe side effects.[A183092] Hydroxychloroquine was granted FDA approval on 18 April 1955.[L8072] |
| PubChem ID: | 3652 |
| CasNo: | 118-42-3 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CCN(CCO)CCCC(C)NC1=C2C=CC(Cl)=CC2=NC=C1 |
| Structure: |
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| InChiKey: | XXSMGPRMXLTPCZ-UHFFFAOYSA-N |
| Molecular Weight: | 335.872 |
| DrugBank Targets: | Toll-like receptor 7; Toll-like receptor 9; DNA; Angiotensin-converting enzyme 2 |
| DrugBank MoA: | The exact mechanisms of hydroxychloroquine are unknown. It has been shown that hydroxychloroquine accumulates in the lysosomes of the malaria parasite, raising the pH of the vacuole.[A183074] This activity interferes with the parasite's ability to proteolyse hemoglobin, preventing the normal growth and replication of the parasite.[A183074] Hydroxychloroquine can also interfere with the action of parasitic heme polymerase, allowing for the accumulation of the toxic product beta-hematin.[A183080] Hydroxychloroquine accumulation in human lysosomes also raises the pH of the vacuole, which inhibits antigen processing, prevents the alpha and beta chains of the major histocompatibility complex (MHC) class II from dimerizing, inhibits antigen presentation of the cell, and reduces the inflammatory response.[A183074] Elevated pH in the vesicles may alter the recycling of MHC complexes so that only the high affinity complexes are presented on the cell surface.[A183074] Self peptides bind to MHC complexes with low affinity and so they will be less likely to be presented to autoimmune T cells.[A183074] Hydroxychloroquine may also reduce the release of cytokines like interleukin-1 and tumor necrosis factor.[A183074] |
| DrugBank Pharmacology: | Hydroxychloroquine affects the function of lysozomes in humans as well as plasmodia.[A183074] Altering the pH of the lysozomes reduces low affinity self antigen presentation in autoimmue diseases and interferes with the ability of plasmodia to proteolyse hemoglobin for their energy requirements.[A183074] Hydroxychloroquine has a long duration of action as it may be taken on a weekly basis for some indications.[L8072] Hydroxychloroquine may lead to severe hypoglycemia and so diabetic patients are advised to monitor their blood glucose levels.[L8072] Hydroxychloroquine is not effective against malaria in areas where chloroquine resistance has been reported.[L8072] |
| DrugBank Indication: | Hydroxychloroquine is indicated for the prophylaxis of malaria where chloroquine resistance is not reported, treatment of uncomplicated malaria (caused by _P. falciparum_, _P. malariae_, _P. ovale_, or _P. vivax_), chronic discoid lupus erythematosus, systemic lupus erythematosus, acute rheumatoid arthritis, and chronic rheumatoid arthritis.[L8072] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L1990 | NCT03081676 | COMPLETED | NO | 2017-03-08 | 2019-06-27 | Details | |
| L2912 | NCT05689372 | NOT_YET_RECRUITING | NO | 2025-03-31 | 2024-09-19 | Details | |
| L2942 | NCT02048189 | PHASE4 | TERMINATED | NO | 2012-03-08 | 2024-02-21 | Details |
| L4685 | NCT00654121 | PHASE2 | COMPLETED | NO | 2000-02 | 2008-04-07 | Details |
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