CA B E N U V A

The N e w a n d Medical
chemistry

Improved
y fo r H IV-
Therap SHABILA LINTANG

1 I n f e c t i o n RAMADHANI
O1A120116
 TABLE OF CONTENT
01 02 03
INTRODUCTIO FORMULATION OF RESULT AND
N THE PROBLEM DISCUSSION

04 05
CONCLUSION REFRENCES
 INTRODUCTION
HIV AIDS is one of many global health problems. The spread of
this deadly virus has threatened not only developed countries,
but also developing countries such as Indonesia.
Combination Antiretroviral therapy can significantly prolong
the life expectancy of people living with human
immunodeficiency virus (HIV), but HIV infection remains a
chronic condition that requires lifelong daily oral treatment.
Two-drug regimens have been developed as an option; long-
acting injectable regimens are another alternative that can
free patients from the burden of daily regimens and potentially
provide a more acceptable therapeutic approach.
  What is The Active

02
Compound?
 What is the active
compound target?
 What is the drug
candidate?
FORMULATION  How is the drug
structure?
OF THE  How is the drugs
synthesis?
PROBLEM
03 The Purpose

 TO DETERMINE THE
ACTIVE COMPOUND OF
DRUGS
 TO DETERMINE THE
DRUG TARGET
 TO DETERMINE THE
DRUG KANDIDATE
 TO DETERMINE THE
DRUG STRUCTURE
RESULT
AND
4.1 CABENUVA Active Compound
CABENUVA contains
cabotegravir extended release
suspension, an HIV INSTI, co
packaged with rilpivirine
extended release injectable
suspension, an HIV NRTI.
Cabotegravir: The chemical name for cabotegravir is (3S,11aR)-N-
[(2,4difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-
hexahydro[1,3] oxazolo[3,2-a] pyrido[1,2-d] pyrazine-8- carboxamide. The empirical
formula is C19H17F2N3O5 and the molecular weight is 405.35 g/mol. It has the
following structural formula:
Rilpivirine: The chemical name for rilpivirine is 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-
dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile. Its molecular formula is
C22H18N6 and its
molecular weight is 366.42.
Cabotegravir extended-
release injectable suspension
is a white to light pink free-
flowing suspension for
intramuscular injection.
Each sterile single-dose vial
contains 2 mL or 3 mL of the
following:
cabotegravir 200 mg/mL
and the following inactive
ingredients: mannitol (35
mg/mL), polyethylene
glycol (PEG) 3350 (20
mg/mL), polysorbate 20 (20
mg/mL), and Water for
Injection.
Rilpivirine extended-
release injectable
suspension is a white to
off-white suspension for
intramuscular injection.
ingredients:
Each sterile single-dose
vial contains 2 mL or 3
mL of the following:
rilpivirine 300 mg/mL
and the following inactive
 4.2 CABENUVA Drugs Target
Bound to human plasma
proteins
A
Plasma concentrations of
B
cabotegravir and rilpivirine
during long-acting therapy (Fig.
2) were similar to the
concentrations reported during
C
oral therapy.1
 4.3 Drug Candidate
Cabotegravir is not a In vitro, cabotegravir was not
clinically relevant a substrate of OATP1B1,
OATP1B3, or OCT1.
inhibitor of the Cabotegravir is a substrate of
following enzymes P-gp and BCRP in vitro;
however, because of its high
and transporters: permeability, no alteration in
cabotegravir absorption is
CYP1A2, 2A6, 2B6, expected with
2C8, 2C9, 2C19, coadministration of P-gp or
BCRP inhibitors. Rilpivirine is
2D6, and 3A4; not likely to have a clinically
UGT1A1, 1A3, 1A4, relevant effect on the exposure
of drugs metabolized by CYP
1A6, 1A9, 2B4, 2B7, enzymes.
2B15, and 2B17
4.4 Drugs Pharmacology

Cabotegravir inhibits HIV

integrase by binding to the
integrase active site and
blocking the strand transfer
step of retroviral
deoxyribonucleic acid (DNA)
integration which is essential
for the HIV replication cycle.
The mean 50% inhibitory
concentration (IC50) value of
cabotegravir in a strand
 Rilpivirin
e is a diar
HIV-1 an ylpyrimid
d inhibits ine NNRT
non-comp HIV-1 re I of
etitive inh plication
reverse tr ibition of by
an HIV-1
not inhib scriptase (RT). Ri
it the hum lp
polymera an cellula ivirine does
ses α, β, a r DNA
nd γ.
4.5 U VA
A BE N
C ES I S
N T H
SY
8

An oral formulation of
cabotegravir (CAB), and
CABENUVA, an extended-
release, injectable, two- drug
copackaged product containing
CAB and rilpivirine (RPV).
CAB is a new integrase strand
transfer inhibitor (INSTI) and
RPV is a previously approved
nonnucleoside reverse
transcriptase inhibitor (NNRTI).
 CONCLUSION

Therapy with long-acting cabotegravir plus rilpivirine was

INFERIOR to oral therapy with dolutegravir–abacavir–
lamivudine with regard to maintaining HIV-1 suppression.
 ● Orkin., dkk. 2020. Long-Acting
Cabotegravir and Rilpivirine after
Oral Induction for HIV-1 Infection.
The new england journal of
medicine :vol 12 no 2
DOI:10.1056/NEJMoa1909512

REFRENCES
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