Investigational Drug Details
| Drug ID: | D548 |
| Drug Name: | Rilpivirine |
| Synonyms: | Complera; Edurant; Juluca; Odefsey |
| Type: | Chemical drug |
| DrugBank ID: | DB08864 |
| DrugBank Description: | Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretrovirals to specifically treat human immunodeficiency virus type 1 (HIV-1). |
| PubChem ID: | -- |
| CasNo: | 500287-72-9 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC1=CC(\C=C\C#N)=CC©=C1NC1=CC=NC(NC2=CC=C(C=C2)C#N)=N1 |
| InChiKey: | YIBOMRUWOWDFLG-ONEGZZNKSA-N |
| Molecular Weight: | 366.4185 |
| DrugBank Targets: | Reverse transcriptase/RNaseH inhibitor; Nuclear receptor subfamily 1 group I member 2 agonist |
| DrugBank MoA: | Rilpivirine is a non-competitive NNRTI that binds to reverse transcriptase.9 Its binding results in the blockage of RNA and DNA- dependent DNA polymerase activities, like HIV-1 replication. It does not present activity against human DNA polymerases α, β and γ. Rilpivirine's flexible structure around the aromatic rings allows the adaptation to changes in the non-nucleoside RT binding pocket, reducing the likelihood of viral mutations conferring resistance. |
| DrugBank Pharmacology: | Rilpivirine is a non-nucleoside reverse transcriptase inhibitor that inhibits the replication of HIV-1. It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly. Patients should be counselled regarding the risk of hypersensitivity reactions, hepatotoxicity, depressive disorders, and the redistribution or accumulation of body fat. |
| DrugBank Indication: | Rilpivirine, in combination with other agents, is indicated for the treatment of HIV-1 infections in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL and CD4+ cell count >200 cells/mm3.6 The FDA combination therapy approval of rilpivirine and dolutegravir is indicated for adults and adolescents 12 years of age and older weighing at least 35 kg with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without a history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy. Rilpivirine in combination with cabotegravir is indicated as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine. |
| Targets: | -- |
| Therapeutic Category: | -- |
| Clinical Trial Progress: | Phase 4 on-going (TCTR20210403003) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0389 | TCTR20210403003 | Phase 4 | Not Recruiting | No Results Available | 03/04/2021 | 7 February 2022 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A02477 | 34359857 | Cells | NNRTI and Liver Damage: Evidence of Their Association and the Mechanisms Involved. | Details |
| A07822 | 32344934 | J Clin Med | Lipidomics Reveals Reduced Inflammatory Lipid Species and Storage Lipids after Switching from EFV/FTC/TDF to RPV/FTC/TDF: A Randomized Open-Label Trial. | Details |
| A10001 | 31530714 | Gut | Rilpivirine attenuates liver fibrosis through selective STAT1-mediated apoptosis in hepatic stellate cells. | Details |
| A14267 | 29493093 | HIV Med | Highlights of the 2017 European AIDS Clinical Society (EACS) Guidelines for the treatment of adult HIV-positive persons version 9.0. | Details |