PHARMACOTHERAPEUTICS-1

ASSIGNMENT
DRUG
PROFILE
SELINEXOR
Robert Selvin M
Pharm 2nd Year
SSMCOP
 WHEN WAS SELINEXOR
APPROVED
On December 18, 2020, the U.S.
Food and Drug Administration
(FDA) approved selinexor
(XPOVIO).
Name Of The
Drug
BRAND :
/ TRADE NAME : GENERIC NAME : CLASSES
• Xpovio • Selinexor : • Selective Inhibitors of
Nuclear Export (SINE)
• Nexpovio

Pharmaceutical Form Of The

Drug
• Tablet
:
Dosage & Structure
Strength : Of Selinexor
• Tablet :
:
• 20 mg
• 40 mg
• 50 mg
• 60 mg

Molecular Formula: C17H11F6N7O

 Indication & Usage
:
Selinexor is a nuclear export inhibitor indicated :

• In combination with dexamethasone for the treatment of adult patients with

relapsed or refractory multiple myeloma who have received at least 4 prior
therapies & whose disease refractory to at least 2 proteasome inhibitors, at
least 2 immuno-modulatory agent & an anti-CD38 monoclonal antibody.

• For the treatment of adult patients with relapsed or refractory diffuse large
B-cell lymphoma [DLBCL] , not otherwise specified , including DLBCL
arising from follicular lymphoma, after at least 2 lines of systemic therapy.
Treatment Duration
:Usual Adult Dose for Multiple
Myeloma
IN COMBINATION WITH BORTEZOMIB AND
DEXAMETHASONE (SVd):
100 mg orally once weekly on Day 1 of each week until disease progression or
unacceptable toxicity in combination with bortezomib 1.3 mg/m2 subcutaneously
once weekly on Day 1 of each week for 4 weeks followed by 1 week off;
dexamethasone 20 mg orally twice weekly on Days 1 and 2 of each week

Usual Adult Dose for

Lymphoma
60 mg orally on Day 1 and 3 of each week until disease progression or
unacceptable toxicity
Pharmacology of drug :
Mechanism of action
• Selective inhibitor of nuclear export (SINE) of tumor suppressor
proteins (TSPs), growth regulators, and mRNAs of oncogenic
proteins by blocking exportin 1 (XPO1)

• XPO1 inhibition leads to accumulation of TSPs in the nucleus,

reductions in several oncoproteins (eg, c–myc, cyclin D1), cell cycle
arrest, and apoptosis of cancer cells

• Selinexor demonstrated proapoptotic activity in vitro in multiple

myeloma cell lines, patient tumor samples, and murine xenograft
model
Absorption
Peak plasma time: 4 hr
• Peak plasma concentration
• 60 mg-dose: 442 ng/mL
• 80 mg-dose: 680 ng/mL
• AUC
• 60 mg-dose: 4,096 ng⋅hr/mL
• 80 mg-dose: 5,386 ng⋅hr/mL
Distribution
• Vd: 133 L
• Protein bound: 95%
Metabolism
Metabolized by CYP3A4, multiple
UGTs, and glutathione S-transferases
Elimination
• Half-life: 6-8 hr
• Clearance: 18.6 L/hr
Warnings And Precautions
:Or Contraindications :
• Thrombocytopenia
• Neutropenia
• Gastrointestinal Toxicity
• Hyponatremia
• Serious Infection
• Neurological Toxicity
• Embryo-Fetal Toxicity
Warning About Use In Pregnancy
& Lactation:
PREGNANC
Y
• Based on animal studies and its mechanism of action, selinexor can
cause fetal harm if administered to pregnant women
• Verify pregnancy status of females of reproductive potential before
initiating selinexor
Animal studies
Administration to pregnant rats during organogenesis resulted in
structural abnormalities and alterations to growth at exposures
below those clinically recommended for humans
 Contraception
• Females of reproductive potential: Use effective contraception during
treatment and for 1 week after the last dose
• Males with female partner of reproductive potential: Use effective
contraception during treatment and for 1 week after the last dose
Infertility
Based on animal studies, selinexor may impair fertility in females & males

LACTATI
ON
• No data are available regarding the presence of selinexor or its metabolites in human
milk, or their effects on the breastfed child or milk production
• Because of the potential for serious adverse reactions in breastfed children, advise
women not to breastfeed during treatment and for 1 week after the last dose
Interactions :
Drug interactions : Other
• Acrivastin • Citalopram inter-
• Adalimumab • Diazepam actions:
• Certain types
• Amiodarone • Fluvoxamine of foods
• Baclofen • Haloperidol • Tobacco
• Buprenorphine • Leflunomide • Alcohol
• Carbamazepine • Methadone
• Ciprofloxacin • Tramadol , etc.
Adverse Drug Reactions
(ADRs):
ADRs in patients with multiple myeloma are ;

• Thrombocytopenia • Vomiting
• Fatigue • Hyponatremia
• Nausea • Neutropenia
• Anemia • Leukopenia
• Decreased appetite • Constipation
• Decreased weight • Dyspnea
• Diarrhea • Upper respiratory
tract infection
ADRs in patients with DLBCL
are ;
• Fatigue • Pyrexia
• Nausea • Thrombocytopenia
• Diarrhea • Lymphopenia
• Appetite decrease • Neutropenia
• Weight decrease • Anemia
• Constipation • Hyponatremia
• Vomiting
Non-Drug Treatment
:
Non-Drug Treatment of Multiple
Myeloma & DLBCL :
Radiation Therapy
Radiation therapy uses high-
powered energy beams from
sources such as X-rays and
protons to kill cancer cells.
 Instructions For Use :
1. Instruct patients to take Selinexor exactly as prescribed.

2. Advise patients that selinexor comes in a child-resistant blister pack.

3. Advise patients to take their prescribed dexamethasone (if applicable) and

prophylactic anti-nausea medications as directed

4. Advise patients that blood tests and body weight will be monitored at
baseline and during treatment as clinically indicated, with more frequent
monitoring during the first three months of treatment.

5. Advise patients to maintain appropriate fluid and caloric intake throughout

their treatment
Administration
: Administration
Oral

• May take with or without food

• Swallow tablet whole; do not break, chew, crush, or divide
• On scheduled administration day, take tablet at about the
same time of day
Missed, delayed, or vomited dose:
• Take next dose at the next regularly scheduled time
• Vomited dose: Do not repeat dose; wait until next scheduled
dose
 Labelling
• : Selinexor [XPOVIO] are blue , round , bi-convex
& film-coated 20mg tablets with “K20” debossed
on one side & nothing on the other side.
• Tablets are packaged in a child-resistant blister
pack.
• Four blister packs are supplied per carton.

Storage:
• Store at or below 30ºC (86ºF)
 BIBLIOGRAP
HY

Internet Source

• FDA.gov • Rxlist.com

• XPOVIO.com • Drugs.com

• Cancer.gov • Medscape.com

• Myeloma.org.uk • Wikipedia
THANK
YOU
Name : Robert Selvin M
Sign :