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Raltegravir potassium

Raltegravir potassium structure

CAS No:
871038-72-1
Formula:
C20H20FN6O5.K
Chemical Name:
Raltegravir potassium
Synonyms:
N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide Potassium Salt;Raltegravir Potassium Salt;MK 0518;Raltegravir potassium;Raltegravir(MK-0518);Raltegravir K;Raltegravir-13C-d3;Raltegravir potassium, >=98%
Categories:
Active Pharmaceutical Ingredients > Synthetic Anti-infective Drugs

Description

Raltegravir (potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.

Raltegravir Potassium is the orally bioavailable potassium salt of a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI) with HIV-1 antiviral activity. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication.|A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.

Raltegravir potassium Basic Attributes

Molecular Weight：

482.511

Exact Mass：

482.111633

EC Number：

1592732-453-0

UNII：

43Y000U234

NCI Thesaurus Code：

C73823

ATC Code：

J05AJ01|J05AR16

HScode：

2934999090

Characteristics

PSA：

153

XLogP3：

2.13150

Appearance：

Off-white solid

Density：

1.46 g/cm3

Melting Point：

155-157°C

Storage Conditions：

-20°C Freezer

Safety Information

Precautionary statement(s)：

P201, P202, P261, P271, P280, P281, P304+P340, P305+P351+P338, P308+P313, P310, P312, P403+P233, P405, P501

Hazard Statements：

H318

GHS Classification：

|Danger|H318 (97.22%): Causes serious eye damage [Danger Serious eye damage/eye irritation]|P201, P202, P261, P271, P280, P281, P304+P340, P305+P351+P338, P308+P313, P310, P312, P403+P233, P405, and P501|Aggregated GHS information provided by 36 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Isentress is indicated in combination with other anti-retroviral medicinal products for the treatment of human immunodeficiency virus (HIV 1) infection.|Dutrebis is indicated in combination with other anti‑retroviral medicinal products for the treatment of human immunodeficiency virus (HIV‑1) infection in adults, adolescents, and children from the age of 6 years and weighing at least 30 kg without present or past evidence of viral resistance to antiviral agents of the InSTI (Integrase Strand Transfer Inhibitor) and NRTI (Nucleoside Reverse Transcriptase Inhibitor) classes (see sections 4.2, 4.4 and 5.1).

MeSH：

Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. (See all compounds classified as Anti-HIV Agents.)|Inhibitors of HIV INTEGRASE, an enzyme required for integration of viral DNA into cellular DNA. (See all compounds classified as HIV Integrase Inhibitors.)

MeSH Entry Terms：

0518, MK

Raltegravir potassium Use and Manufacturing

Uses

A potent human immunodeficiency virus (HIV) integrase inhibitor.A novel anti-AIDS drug

Use Classification：

Human drugs -> Isentress -> EMA Drug Category|Antivirals for systemic use -> Human pharmacotherapeutic group|Human drugs -> Dutrebis -> EMA Drug Category|Antivirals for systemic use, Antivirals for treatment of HIV infections, combinations -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:482.5
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:6
Exact Mass:482.11162741
Monoisotopic Mass:482.11162741
Topological Polar Surface Area:153
Heavy Atom Count:33
Complexity:843
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Raltegravir is not a substrate for cytochrome P450 (CYP) enzymes and does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 or CYP3A in vitro; it does not induce CYP3A4. Raltegravir is mainly metabolized and eliminated through the glucuronidation pathway mediated by UGT1A1. Caution should be exercised when used in combination with strong inducers of UGT1A1 (such as rifampicin), which may reduce the blood concentration of raltegravir; when used in combination with strong inhibitors of UGT1A1 (such as atazanavir), the blood concentration may be increased, but no dose adjustment is required.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Raltegravir Potassium Tablets
Specifications	400mg (based on raltegravir)

Raltegravir Potassium Tablets
Specifications	400 mg (based on raltegravir)

Raltegravir Potassium Tablets
Specifications	400mg (based on raltegravir)

See More Related Drugs

Registered Holders

MATRIX PHARMACORP PRIVATE LTD

United States
Active
MATRIX PHARMACORP PRIVATE LIMITED

European Union
Active
SHANGHAI DESANO CHEMICAL PHARMACEUTICAL CO., LTD.

European Union
Active

See More Registered Holders

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