KP-1461
KP-1461 Uses, Dosage, Side Effects, Food Interaction and all others data.
KP-1461 is a potent, non-chain-terminating, mutagenic deoxyribonucleoside analogue. Designated a DNA covert nucleoside, the drug consists of a modified base that incorporates randomly into HIV and pairs with multiple bases.
Trade Name | KP-1461 |
Generic | KP-1461 |
Type | |
Formula | C16H28N4O6 |
Weight | Average: 372.422 Monoisotopic: 372.200884638 |
Groups | Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Investigated for use/treatment in HIV infection.
How KP-1461 works
KP-1461 is the oral prodrug of KP-1212. KP-1461 is also known as SN1212. KP-1461 introduces continual mutations into HIV during viral replication by reverse transcriptase (RT). These mutations decrease virus viability and are eventually lethal. This mechanism, selective viral mutagenesis or lethal mutagenesis, is novel to the nucleoside analogue class. Unlike approved nucleoside RT inhibitors (NRTIs) that contain a modified sugar and unmodified base, KP-1461 has a modified base that allows multiple base pairing. Because KP-1461 pairs with multiple bases, it is able to target all viral proteins rather than a single protein. KP-1461, after conversion to KP-1212, is metabolized to a triphosphate and incorporated into the HIV-1 genome by RT. The drug is similarly incorporated into human mitochondrial DNA polymerase. The active substance KP-1212 has been shown to inhibit antiviral activity in tissues after just one pass; accumulation has been shown to eradicate the virus entirely. HIV strains treated with KP-1212 also showed increased sensitivity to zidovudine.
Innovators Monograph
You find simplified version here KP-1461