Selexipag- Uptravi (Dec 2015)- Antihypertensives
Drug Name:Selexipag- Uptravi (Dec 2015)- Antihypertensives
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Strong CYP2C8 inhibitors: increased exposure to selexipag and its active
metabolite. Avoid concomitant use.
Indication:
UPTRAVIR (selexipag) tablets, for oral use
Initial U.S. Approval: 2015
NEW MOLECULAR ENTITY AND NEW THERAPEUTIC BIOLOGICAL
PRODUCTS APPROVED FOR 2015
Certain drugs are classified as New molecular Emtities- NME- for FDA review
Many of these products contain active moieties that have not been approved
by FDA previously, either as a single ingredient or as part of a combination
products; these products frequently provide important new therapies for the
patients.
Some drugs are characterized as NMEs for administrative purposes ,but
nonetheless contain certain active moieties in products that have been
previously approved by FDA. For example, CDER classifies biological
products submitted in an application under section 351(a) of the Public
Service Act as NME for purposes of FDA review, regardless of whether
the agency previously approved a related active moiety in a different
product.
FDAs classification of a drug as an -NME- for review purposes is distinct
from FDAs determination of whether a drug is a - New Chemical Entity or - NCE-
within the meaning of the Federal Food,Drug, and Cosmetic Act
No.44
Drug Name - Selexipag
Active Ingredient- Uptravi
Date of approval - 12/22/2015
FDA-approved use - To treat pulmonary arterial hypertension
Approved by US FDA on 12/22/2015- (Ref- FDA approved List- 2015)
Adverse Reaction:
Adverse reactions occurring more frequently (>5%) on UPTRAVI compared
to placebo are headache, diarrhea, jaw pain, nausea, myalgia, vomiting,
pain in extremity, and flushing.
Contra-Indications:
CONTRAINDICATIONS
None
WARNINGS AND PRECAUTIONS
Pulmonary edema in patients with pulmonary veno-occlusive disease.
If confirmed, discontinue treatment.
Dosages/ Overdosage Etc:
INDICATIONS AND USAGE
UPTRAVIR is a prostacyclin receptor agonist indicated for the treatment
of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease
progression and reduce the risk of hospitalization for PAH.
DOSAGE AND ADMINISTRATION
Starting dose: 200 mcg twice daily.
Increase the dose by 200 mcg twice daily at weekly intervals to
the highest tolerated dose up to 1600 mcg twice daily.
Maintenance dose is determined by tolerability.
Moderate hepatic impairment: Starting dose 200 mcg once daily,
increase the dose by 200 mcg once daily at weekly intervals to the highest
tolerated dose up to 1600 mcg.
DOSAGE FORMS AND STRENGTHS
Tablets: 200 mcg, 400 mcg, 600 mcg, 800 mcg,
1000 mcg, 1200 mcg, 1400 mcg, 1600 mcg.
Patient Information:
PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Patient Package Insert).
Inform patients:
what to do if they miss a dose
not to split, crush, or chew tablets.
Manufactured for: Actelion Pharmaceuticals US, Inc.
5000 Shoreline Court, Ste. 200 South San Francisco, CA 94080, USA ACT20151221
2015 Actelion Pharmaceuticals US, Inc
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1. Mechanism of Action
Selexipag is an oral prostacyclin receptor (IP receptor) agonist that is structurally
distinct from prostacyclin. Selexipag is hydrolyzed by carboxylesterase 1 to yield
its active metabolite, which is approximately 37-fold as potent as selexipag.
Selexipag and the active metabolite are selective for the IP receptor versus other
prostanoid receptors (EP1-4, DP, FP and TP).
2 Pharmacokinetics
The pharmacokinetics of selexipag and its active metabolite have been studied
primarily in healthy subjects. The pharmacokinetics of selexipag and the active
metabolite, after both single-and multiple-dose administration, were
dose-proportional up to a single dose of 800 mcg and multiple doses of up to
1800 mcg twice daily.
No accumulation in plasma, either of parent compound or active metabolite,
occurred after multiple-dose administration
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Risk Summary
There are no adequate and well-controlled studies with UPTRAVI in pregnant women.
2. Lactation
It is not known if UPTRAVI is present in human milk. Selexipag or its metabolites
were present in the milk of rats. Because many drugs are present in the human milk
and because of the potential for serious adverse reactions in nursing infants,
discontinue nursing or discontinue UPTRAVI.
3. Pediatric Use
Safety and effectiveness in pediatric patients have not been established.
4. Geriatric Use
Of the 1368 subjects in clinical studies of UPTRAVI 248 subjects were 65 years of age
and older, while 19 were 75 and older.
No overall differences were observed between these subjects and younger subjects,
and other reported clinical experience has not identified differences in response
between the elderly and younger patients, but greater sensitivity cannot be ruled out.
