What is the dosage of Retevmo?

Retevmo is available in 6 dosages, including 120 mg Tab, 40 mg Tab, 80 mg Cap, 160 mg Tab, 80 mg Tab and 40 mg Cap

What does Retevmo treat?

Retevmo treats Carcinoma, Non-Small-Cell Lung and Thyroid Neoplasms

What is Retevmo made of?

Retevmo contains selpercatinib which is a Kinase Inhibitor

How is Retevmo administered?

Retevmo is administered as a Oral Pill

What is Retevmo mechanism of action?

Retevmo mechanism of action is P-Glycoprotein Inhibitors, Cytochrome P450 2C8 Inhibitors, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A Inhibitors, Multidrug and Toxin Extrusion Transporter 1 Inhibitors or Rearranged during Transfection (RET) Inhibitors

Retevmo

(selpercatinib)

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Dosage & Administration

* Select patients for treatment with RETEVMO based on the presence of a RET gene fusion (NSCLC, thyroid, or other solid tumors) or specific RET gene mutation (MTC).
* Adult and adolescent patients 12 years of age or older:
the recommended dosage is based on weight :
* Less than 50 kg: 120 mg orally twice daily
* 50 kg or greater: 160 mg orally twice daily

* Pediatric patients 2 to less than 12 years of age:
the recommended dosage is based on body surface area :
* 0.33 to 0.65 m2: 40 mg orally three times daily
* 0.66 to 1.08 m2: 80 mg orally twice daily
* 1.09 to 1.52 m2: 120 mg orally twice daily
* ≥1.53 m2: 160 mg orally twice daily

* Reduce RETEVMO dose in patients with severe hepatic impairment.

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Retevmo Prescribing Information

RET Fusion-Positive Non-Small Cell Lung Cancer

RETEVMO® is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test.

RET-Mutant Medullary Thyroid Cancer

RETEVMO is indicated for the treatment of adult and pediatric patients 2 years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy.

RET Fusion-Positive Thyroid Cancer

RETEVMO is indicated for the treatment of adult and pediatric patients 2 years of age and older with advanced or metastatic thyroid cancer with a RET gene fusion, as detected by an FDA-approved test, who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate).

Other RET Fusion-Positive Solid Tumors

RETEVMO is indicated for the treatment of adult and pediatric patients 2 years of age and older with locally advanced or metastatic solid tumors with a RET gene fusion, as detected by an FDA-approved test, that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options.

This indication is approved under accelerated approval based on overall response rate and duration of response [see Clinical Studies ]. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s).

Patient Selection

Select patients for treatment with RETEVMO based on the presence of a RET gene fusion (NSCLC, thyroid cancer, or other solid tumors) or specific RET gene mutation (MTC) in tumor specimens [see Clinical Studies ]. Information on FDA-approved test(s) for the detection of RET gene fusions and RET gene mutations is available at: http://www.fda.gov/CompanionDiagnostics. An FDA-approved companion diagnostic test for the detection of RET gene fusions and RET gene mutations in plasma is not available.

Important Administration Instructions

RETEVMO may be taken with or without food unless coadministered with a proton pump inhibitor (PPI) [see Dosage and Administration ].

Recommended Dosage

The recommended dosage of RETEVMO is shown in Table 1:

Table 1: Recommended RETEVMO Dosage
Population	RETEVMO Dosage
Adult and adolescent patients 12 years of age or older based on body weight
Less than 50 kg	120 mg twice daily
50 kg or greater	160 mg twice daily
Pediatric patients 2 to less than 12 years of age based on body surface area
0.33 to 0.65 m2	40 mg three times daily
0.66 to 1.08 m2	80 mg twice daily
1.09 to 1.52 m2	120 mg twice daily
≥1.53 m2	160 mg twice daily
Dosing pediatric patients with body surface area less than 0.33 m2 is not recommended

Continue treatment with RETEVMO until disease progression or unacceptable toxicity.

Swallow the capsules whole. Do not crush or chew the capsules. Do not administer to pediatric patients who are unable to swallow a capsule.

Swallow the tablets whole. Do not crush or chew the tablets.

Do not take a missed dose unless it is more than 6 hours until next scheduled dose.

If vomiting occurs after RETEVMO administration, do not take an additional dose and continue to the next scheduled time for the next dose.

Dosage Modifications for Concomitant Use of Acid-Reducing Agents

Avoid concomitant use of a PPI, a histamine-2 (H2) receptor antagonist, or a locally-acting antacid with RETEVMO [see Drug Interactions ]. If concomitant use cannot be avoided:

Take RETEVMO with food when coadministered with a PPI.
Take RETEVMO 2 hours before or 10 hours after administration of an H2 receptor antagonist.
Take RETEVMO 2 hours before or 2 hours after administration of a locally-acting antacid.

Dosage Modifications for Adverse Reactions

The recommended dose reductions for adverse reactions are provided in Table 2.

Table 2: Recommended RETEVMO Dose Reductions for Adverse Reactions
Current RETEVMO Dosage	Dose Reduction
Current RETEVMO Dosage	First	Second	Third
40 mg three times daily	40 mg twice daily	40 mg once daily	permanently discontinue
80 mg twice daily	40 mg twice daily	40 mg once daily	permanently discontinue
120 mg twice daily	80 mg twice daily	40 mg twice daily	40 mg once daily
160 mg twice daily	120 mg twice daily	80 mg twice daily	40 mg twice daily
Permanently discontinue RETEVMO in patients unable to tolerate three dose reductions.

The recommended dosage modifications for adverse reactions are provided in Table 3.

Table 3: Recommended RETEVMO Dosage Modifications for Adverse Reactions
Adverse Reaction	Severity	Dosage Modification
Hepatotoxicity [see Warnings and Precautions ]	Grade 3 or Grade 4	Withhold RETEVMO and monitor AST/ALT once weekly until resolution to Grade 1 or baseline. Resume at reduced dose by 2 dose levels and monitor AST and ALT once weekly until 4 weeks after reaching dose taken prior to the onset of Grade 3 or 4 increased AST or ALT. Increase dose by 1 dose level after a minimum of 2 weeks without recurrence and then increase to dose taken prior to the onset of Grade 3 or 4 increased AST or ALT after a minimum of 4 weeks without recurrence.
Interstitial Lung Disease/ Pneumonitis [see Warnings and Precautions ]	Grade 2	Withhold RETEVMO until resolution. Resume at a reduced dose. Discontinue RETEVMO for recurrent ILD/pneumonitis.
	Grade 3 or Grade 4	Discontinue RETEVMO for confirmed ILD/pneumonitis.
Hypertension [see Warnings and Precautions ]	Grade 3	Withhold RETEVMO for Grade 3 hypertension that persists despite optimal antihypertensive therapy. Resume at a reduced dose when hypertension is controlled.
Hypertension [see Warnings and Precautions ]	Grade 4	Discontinue RETEVMO.
QT Interval Prolongation [see Warnings and Precautions ]	Grade 3	Withhold RETEVMO until recovery to baseline or Grade 0 or 1. Resume at a reduced dose or permanently discontinue RETEVMO.
QT Interval Prolongation [see Warnings and Precautions ]	Grade 4	Discontinue RETEVMO.
Hemorrhagic Events [see Warnings and Precautions ]	Grade 3 or Grade 4	Withhold RETEVMO until recovery to baseline or Grade 0 or 1. Discontinue RETEVMO for severe or life-threatening hemorrhagic events.
Hypersensitivity Reactions [see Warnings and Precautions ]	All Grades	Withhold RETEVMO until resolution of the event. Initiate corticosteroids. Resume at a reduced dose by 3 dose levels while continuing corticosteroids. Increase dose by 1 dose level each week until the dose taken prior to the onset of hypersensitivity is reached, then taper corticosteroids.
Hypothyroidism [see Warnings and Precautions ]	Grade 3 or Grade 4	Withhold RETEVMO until resolution to Grade 1 or baseline. Discontinue RETEVMO based on severity.
Other Adverse Reactions [see Adverse Reactions ]	Grade 3 or Grade 4	Withhold RETEVMO until recovery to baseline or Grade 0 or 1. Resume at a reduced dose.

Dosage Modifications for Concomitant Use of Strong and Moderate CYP3A Inhibitors

Avoid concomitant use of strong and moderate CYP3A inhibitors with RETEVMO. If concomitant use of a strong or moderate CYP3A inhibitor cannot be avoided, reduce the RETEVMO dose as recommended in Table 4. After the inhibitor has been discontinued for 3 to 5 elimination half-lives, resume RETEVMO at the dose taken prior to initiating the CYP3A inhibitor [see Drug Interactions ].

Table 4: Recommended RETEVMO Dosage for Concomitant Use of Strong and Moderate CYP3A Inhibitors
Current RETEVMO Dosage	Recommended RETEVMO Dosage
	Moderate CYP3A Inhibitor	Strong CYP3A Inhibitor
40 mg orally three times daily	40 mg orally once daily	40 mg orally once daily
80 mg orally twice daily	40 mg orally twice daily	40 mg orally twice daily
120 mg orally twice daily	80 mg orally twice daily	40 mg orally twice daily
160 mg orally twice daily	120 mg orally twice daily	80 mg orally twice daily

Dosage Modification for Severe Hepatic Impairment

Reduce the recommended dosage of RETEVMO for patients with severe hepatic impairment as recommended in Table 5 [see Use in Specific Populations ].

Table 5: Recommended RETEVMO Dosage for Severe Hepatic Impairment
Current RETEVMO Dosage	Recommended RETEVMO Dosage
40 mg orally three times daily	40 mg orally twice daily
80 mg orally twice daily	40 mg orally twice daily
120 mg orally twice daily	80 mg orally twice daily
160 mg orally twice daily	80 mg orally twice daily

Capsules:

40 mg: gray opaque capsule imprinted with “Lilly”, “3977” and “40 mg” in black ink.
80 mg: blue opaque capsule imprinted with “Lilly”, “2980” and “80 mg” in black ink.

Tablets:

40 mg: light gray, film coated, round tablet debossed with “Ret 40” on one side and “5340” on the other side.
80 mg: dark red-purple, film coated, round tablet debossed with “Ret 80” on one side and “6082” on the other side.
120 mg: light purple, film coated, round tablet debossed with “Ret 120” on one side and “6120” on the other side.
160 mg: light pink, film coated, round tablet debossed with “Ret 160” on one side and “5562” on the other side.

Pregnancy

Risk Summary

Based on findings from animal studies, and its mechanism of action [see Clinical Pharmacology ], RETEVMO can cause fetal harm when administered to a pregnant woman. There are no available data on RETEVMO use in pregnant women to inform drug-associated risk. Administration of selpercatinib to pregnant rats during the period of organogenesis resulted in embryolethality and malformations at maternal exposures that were approximately equal to the human exposure at the clinical dose of 160 mg twice daily. Advise pregnant women of the potential risk to a fetus.

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Data

Animal Data

Selpercatinib administration to pregnant rats during the period of organogenesis at oral doses ≥100 mg/kg [approximately 3.6 times the human exposure based on the area under the curve (AUC) at the clinical dose of 160 mg twice daily] resulted in 100% post-implantation loss. At the dose of 50 mg/kg [approximately equal to the human exposure (AUC) at the clinical dose of 160 mg twice daily], 6 of 8 females had 100% early resorptions; the remaining 2 females had high levels of early resorptions with only 3 viable fetuses across the 2 litters. All viable fetuses had decreased fetal body weight and malformations (2 with short tail and one with small snout and localized edema of the neck and thorax).

Lactation

Risk Summary

There are no data on the presence of selpercatinib or its metabolites in human milk or on their effects on the breastfed child or on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with RETEVMO and for 1 week after the last dose.

Females and Males of Reproductive Potential

Based on animal data, RETEVMO can cause embryolethality and malformations at doses resulting in exposures less than or equal to the human exposure at the clinical dose of 160 mg twice daily [see Use in Specific Populations ].

Pregnancy Testing

Verify pregnancy status in females of reproductive potential prior to initiating RETEVMO [see Use in Specific Populations ].

Contraception

Females

Advise female patients of reproductive potential to use effective contraception during treatment with RETEVMO and for 1 week after the last dose.

Males

Advise males with female partners of reproductive potential to use effective contraception during treatment with RETEVMO and for 1 week after the last dose.

Infertility

RETEVMO may impair fertility in females and males of reproductive potential [see Use in Specific Populations , Nonclinical Toxicology ].

Pediatric Use

The safety and effectiveness of RETEVMO have been established in pediatric patients 2 years of age and older for the treatment of:

advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation who require systemic therapy
advanced or metastatic thyroid cancer with a RET gene fusion who require systemic therapy and are radioactive iodine-refractory (if radioactive iodine is appropriate)
locally advanced or metastatic solid tumors with a RET gene fusion that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options.

Use of RETEVMO for these indications is supported by evidence from adequate and well-controlled studies in adult and pediatric patients with additional pharmacokinetic and safety data in pediatric patients 2 years of age and older [see Adverse Reactions , Clinical Pharmacology , Clinical Studies ]. The predicted exposures of selpercatinib in pediatric patients at the recommended dosages were within the range of values predicted in patients ≥ 12 years and ≥ 50 kg in body weight receiving the approved recommended dosage of 160 mg twice daily [see Clinical Pharmacology ].

The safety and effectiveness of RETEVMO have not been established in these indications in patients less than 2 years of age.

The safety and effectiveness of RETEVMO have not been established in pediatric patients for other indications [see Indications and Usage ].

Juvenile Animal Toxicity Data

In a juvenile rat toxicity study, animals were dosed daily with selpercatinib from post-natal day 21 to day 70 (approximately equivalent to a human child to late adolescent). Selpercatinib increased physeal thickness of multiple bones, extending into the metaphysis and associated with decreased trabecular bone, which was not reversible at doses approximately equivalent to or greater than the adult human exposure at the clinical dose of 160 mg twice daily. Growth plate changes were associated with impairment of bone modeling, resulting in decreased femur length and with reduction in bone mineral density. Selpercatinib also induced reversible hypocellularity of bone marrow in males at ≥30 mg/kg (approximately equivalent to or greater than the adult human exposure at the clinical dose of 160 mg twice daily), and reversible alterations of dentin composition at ≥50 mg/kg (approximately 3 times the adult human exposure at the clinical dose of 160 mg twice daily). Irreversible, dose-dependent degeneration of testicular germinal epithelium, with vacuolation of Sertoli cells and corresponding depletion of spermatozoa in the epididymides, was also observed at ≥ 30 mg/kg (approximately equivalent to or greater than the adult human exposure at the clinical dose of 160 mg twice daily) and affected male reproductive performance at 50 mg/kg (approximately 3 times the adult human exposure at the clinical dose of 160 mg twice daily). Females exhibited delay in attainment of vaginal patency, a marker of sexual maturity, at 125 mg/kg (approximately 4 times the adult human exposure at the clinical dose of 160 mg twice daily); this effect was associated with lower mean body weight. Similar effects in irregular thickening of growth plates in adult rats and minipigs, and tooth dysplasia and malocclusion, resulting in tooth loss in adult rats were observed in repeat dose studies of up to 13-week duration with selpercatinib.

Monitor growth plates in pediatric patients with open growth plates. Consider interrupting or discontinuing therapy based on the severity of any growth plate abnormalities and based on an individual risk-benefit assessment.

Geriatric Use

Of 796 patients who received RETEVMO, 34% (268 patients) were ≥65 years of age and 9% (74 patients) were ≥75 years of age. No overall differences were observed in the safety or effectiveness of RETEVMO between patients who were ≥65 years of age and younger patients.

Renal Impairment

No dosage modification is recommended for patients with mild to severe renal impairment [estimated Glomerular Filtration Rate (eGFR) ≥15 to 89 mL/min, estimated by Modification of Diet in Renal Disease (MDRD) equation]. The recommended dosage has not been established for patients with end-stage renal disease (ESRD) [see Clinical Pharmacology ].

Hepatic Impairment

Reduce the dose when administering RETEVMO to patients with severe [total bilirubin greater than 3 to 10 times upper limit of normal (ULN) and any AST] hepatic impairment [see Dosage and Administration ]. No dosage modification is recommended for patients with mild (total bilirubin less than or equal to ULN with AST greater than ULN or total bilirubin greater than 1 to 1.5 times ULN with any AST) or moderate (total bilirubin greater than 1.5 to 3 times ULN and any AST) hepatic impairment. Monitor for RETEVMO-related adverse reactions in patients with hepatic impairment [see Clinical Pharmacology ].

Hepatotoxicity

Serious hepatic adverse reactions occurred in 3% of patients treated with RETEVMO. Increased AST occurred in 59% of patients, including Grade 3 or 4 events in 11% and increased ALT occurred in 55% of patients, including Grade 3 or 4 events in 12% [see Adverse Reactions ]. The median time to first onset for increased AST was 6 weeks (range: 1 day to 3.4 years) and increased ALT was 5.8 weeks (range: 1 day to 2.5 years).

Monitor ALT and AST prior to initiating RETEVMO, every 2 weeks during the first 3 months, then monthly thereafter and as clinically indicated. Withhold, reduce the dose or permanently discontinue RETEVMO based on the severity [see Dosage and Administration ].

Interstitial Lung Disease/Pneumonitis

Severe, life-threatening, and fatal interstitial lung disease (ILD)/pneumonitis can occur in patients treated with RETEVMO. ILD/pneumonitis occurred in 1.8% of patients who received RETEVMO, including 0.3% with Grade 3 or 4 events, and 0.3% with fatal reactions.

Monitor for pulmonary symptoms indicative of ILD/pneumonitis. Withhold RETEVMO and promptly investigate for ILD in any patient who presents with acute or worsening of respiratory symptoms which may be indicative of ILD (e.g., dyspnea, cough, and fever). Withhold, reduce the dose or permanently discontinue RETEVMO based on severity of confirmed ILD [see Dosage and Administration ].

Hypertension

Hypertension occurred in 41% of patients, including Grade 3 hypertension in 20% and Grade 4 in one (0.1%) patient [see Adverse Reactions ]. Overall, 6.3% had their dose interrupted and 1.3% had their dose reduced for hypertension. Treatment-emergent hypertension was most commonly managed with anti-hypertension medications.

Do not initiate RETEVMO in patients with uncontrolled hypertension. Optimize blood pressure prior to initiating RETEVMO. Monitor blood pressure after 1 week, at least monthly thereafter and as clinically indicated. Initiate or adjust anti-hypertensive therapy as appropriate. Withhold, reduce the dose, or permanently discontinue RETEVMO based on the severity [see Dosage and Administration ].

QT Interval Prolongation

RETEVMO can cause concentration-dependent QT interval prolongation [see Clinical Pharmacology ]. An increase in QTcF interval to >500 ms was measured in 7% of patients and an increase in the QTcF interval of at least 60 ms over baseline was measured in 20% of patients [see Adverse Reactions ]. RETEVMO has not been studied in patients with clinically significant active cardiovascular disease or recent myocardial infarction.

Monitor patients who are at significant risk of developing QTc prolongation, including patients with known long QT syndromes, clinically significant bradyarrhythmias, and severe or uncontrolled heart failure. Assess QT interval, electrolytes and TSH at baseline and periodically during treatment, adjusting frequency based upon risk factors including diarrhea. Correct hypokalemia, hypomagnesemia, and hypocalcemia prior to initiating RETEVMO and during treatment.

Monitor the QT interval more frequently when RETEVMO is concomitantly administered with strong and moderate CYP3A inhibitors or drugs known to prolong QTc interval. Withhold and reduce the dose or permanently discontinue RETEVMO based on the severity [see Dosage and Administration ].

Hemorrhagic Events

Serious including fatal hemorrhagic events can occur with RETEVMO. Grade ≥3 hemorrhagic events occurred in 3.1% of patients treated with RETEVMO, including 4 (0.5%) patients with fatal hemorrhagic events, including cerebral hemorrhage (n = 2), tracheostomy site hemorrhage (n = 1), and hemoptysis (n=1).

Permanently discontinue RETEVMO in patients with severe or life-threatening hemorrhage [see Dosage and Administration ].

Hypersensitivity

Hypersensitivity occurred in 6% of patients receiving RETEVMO, including Grade 3 hypersensitivity in 1.9%. The median time to onset was 1.9 weeks (range: 5 days to 2 years). Signs and symptoms of hypersensitivity included fever, rash and arthralgias or myalgias with concurrent decreased platelets or transaminitis.

If hypersensitivity occurs, withhold RETEVMO and begin corticosteroids at a dose of 1 mg/kg prednisone (or equivalent). Upon resolution of the event, resume RETEVMO at a reduced dose and increase the dose of RETEVMO by 1 dose level each week as tolerated until reaching the dose taken prior to onset of hypersensitivity [see Dosage and Administration ]. Continue steroids until patient reaches target dose and then taper. Permanently discontinue RETEVMO for recurrent hypersensitivity.

Tumor Lysis Syndrome

Tumor lysis syndrome (TLS) occurred in 0.6% of patients with medullary thyroid carcinoma receiving RETEVMO [see Adverse Reactions ]. Patients may be at risk of TLS if they have rapidly growing tumors, a high tumor burden, renal dysfunction, or dehydration. Closely monitor patients at risk, consider appropriate prophylaxis including hydration, and treat as clinically indicated.

Risk of Impaired Wound Healing

Impaired wound healing can occur in patients who receive drugs that inhibit the vascular endothelial growth factor (VEGF) signaling pathway. Therefore, RETEVMO has the potential to adversely affect wound healing.

Withhold RETEVMO for at least 7 days prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing. The safety of resumption of RETEVMO after resolution of wound healing complications has not been established.

Hypothyroidism

RETEVMO can cause hypothyroidism. Hypothyroidism occurred in 13% of patients treated with RETEVMO; all reactions were Grade 1 or 2. Hypothyroidism occurred in 13% of patients (50/373) with thyroid cancer and 13% of patients (53/423) with other solid tumors including NSCLC [see Adverse Reactions ].

Monitor thyroid function before treatment with RETEVMO and periodically during treatment. Treat with thyroid hormone replacement as clinically indicated. Withhold RETEVMO until clinically stable or permanently discontinue RETEVMO based on severity [see Dosage and Administration ].

Embryo-Fetal Toxicity

Based on data from animal reproduction studies and its mechanism of action, RETEVMO can cause fetal harm when administered to a pregnant woman. Administration of selpercatinib to pregnant rats during organogenesis at maternal exposures that were approximately equal to those observed at the recommended human dose of 160 mg twice daily resulted in embryolethality and malformations.

Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with RETEVMO and for 1 week after the last dose. Advise males with female partners of reproductive potential to use effective contraception during treatment with RETEVMO and for 1 week after the last dose [see Use in Specific Populations ].

Slipped Capital Femoral Epiphysis/Slipped Upper Femoral Epiphysis in Pediatric Patients

Slipped capital femoral epiphysis/slipped upper femoral epiphysis (SCFE/SUFE) occurred in 1 adolescent (3.7% of 27 patients) receiving RETEVMO in LIBRETTO-121 and 1 adolescent (0.5% of 193 patients) receiving RETEVMO in LIBRETTO-531 [see Adverse Reactions ]. Monitor patients for symptoms indicative of SCFE/SUFE and treat as medically and surgically appropriate [see Adverse Reactions ].