Raltegravir

Category: pharmacological

Aliases: Isentress

Pharmacological Mechanism

First-in-class HIV integrase strand-transfer inhibitor (INSTI) — blocks viral DNA integration into host genome. Largely supplanted by dolutegravir + bictegravir for once-daily dosing + better resistance barrier.

Half-Life (t½)

PO: 9h

Dosing Guidelines

• PO: Typical 400 mg (Range: 400–800 mg)

Target Organ Systems

• immune-hematologic

Pathways It Modulates

• HIV replication cycle blockade (inhibitor) — HIV-1 integrase (strand transfer)

Chemical Identifiers

• PubChem CID: 54671008
• Formula: C20H21FN6O5
• Molecular weight: 444.42 g/mol
• InChIKey: CZFFBEXEKNGXKS-UHFFFAOYSA-N
• SMILES: CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F

References

• PMID 27696440