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Retevmo

Last reviewed on RxList: 9/16/2020
Retevmo Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Retevmo?

Retevmo (selpercatinib) is a kinase inhibitor used to treat adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC), adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC) who require systemic therapy, and adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate).

What Are Side Effects of Retevmo?

Side effects of Retevmo include:

Dosage for Retevmo

The recommended dosage of Retevmo in adults and pediatric patients 12 years of age or older is based on weight. For weight less than 50 kg: 120 mg orally twice daily; for weight 50 kg or greater: 160 mg orally twice daily.

Retevmo In Children

The safety and effectiveness of Retevmo have been established in pediatric patients aged 12 years and older for medullary thyroid cancer (MTC) who require systemic therapy and for advanced RET fusion-positive thyroid cancer who require systemic therapy and are radioactive iodine-refractory (if radioactive iodine is appropriate).

The safety and effectiveness of Retevmo have not been established in pediatric patients for other indications.

What Drugs, Substances, or Supplements Interact with Retevmo?

Retevmo may interact with other medicines such as:

  • acid-reducing agents (such as proton pump inhibitors, H2 receptor antagonists, and locally-acting antacids),
  • strong and moderate CYP3A inhibitors or inducers,
  • CYP2C8 and CYP3A substrates, and
  • medications known to prolong the QT interval

Tell your doctor all medications and supplements you use.

Retevmo During Pregnancy and Breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant before using Retevmo; it may harm a fetus. Female patients of reproductive potential and males with female partners of reproductive potential are advised to use effective contraception during treatment with Retevmo and for 1week after the final dose. It is unknown if Retevmo passes into breast milk. Because of the potential for serious adverse reactions in breastfed children, breastfeeding is not recommended while using Retevmo and for 1 week after the final dose.

Additional Information

Our Retevmo (selpercatinib) Capsules, for Oral Use Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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Retevmo Consumer Information

Get emergency medical help if you have signs of an allergic reaction: hives, rash; fever, joint or muscle pain; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • easy bruising or bleeding (nosebleeds, bleeding gums);
  • coughing up blood or vomit that looks like coffee grounds;
  • any wound that will not heal;
  • fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness (like you might pass out);
  • fever, chills, cough with mucus, chest pain, feeling short of breath; or
  • liver problems--loss of appetite, stomach pain (upper right side), dark urine, jaundice (yellowing of the skin or eyes).

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

Common side effects may include:

  • abnormal blood tests;
  • high blood pressure;
  • tiredness;
  • dry mouth;
  • diarrhea;
  • swelling;
  • rash; or
  • constipation.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Retevmo (Selpercatinib Capsules)

QUESTION

Lung cancer is a disease in which lung cells grow abnormally in an uncontrolled way. See Answer
Retevmo Professional Information

SIDE EFFECTS

The following clinically significant adverse reactions are described elsewhere in the labeling:

  • Hepatotoxicity [see WARNINGS AND PRECAUTIONS]
  • Hypertension [see WARNINGS AND PRECAUTIONS]
  • QT Interval Prolongation [see WARNINGS AND PRECAUTIONS]
  • Hemorrhagic Events [see WARNINGS AND PRECAUTIONS]
  • Hypersensitivity [see WARNINGS AND PRECAUTIONS]
  • Risk of Impaired Wound Healing [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

RET Gene Fusion Or Gene Mutation Positive Solid Tumors

The pooled safety population described in the WARNINGS and PRECAUTIONS and below reflects exposure to RETEVMO as a single agent at 160 mg orally twice daily evaluated in 702 patients in LIBRETTO-001 [see Clinical Studies]. Among the 702 patients who received RETEVMO, 65% were exposed for 6 months or longer and 34% were exposed for greater than one year. Among these patients, 95% received at least one dose of RETEVMO at the recommended dosage of 160 mg orally twice daily.

The median age was 59 years (range: 15 to 92 years); 0.3% were pediatric patients 12 to 16 years of age; 52% were male; and 69% were White, 22% were Asian, 5% were Hispanic/Latino, and 3% were Black. The most common tumors were NSCLC (47%), MTC (44%), and nonmedullary thyroid carcinoma (5%).

Serious adverse reactions occurred in 33% of patients who received RETEVMO. The most frequent serious adverse reaction (in ≥ 2% of patients) was pneumonia. Fatal adverse reactions occurred in 3% of patients; fatal adverse reactions which occurred in > 1 patient included sepsis (n = 3), cardiac arrest (n = 3) and respiratory failure (n = 3).

Permanent discontinuation due to an adverse reaction occurred in 5% of patients who received RETEVMO. Adverse reactions resulting in permanent discontinuation included increased ALT (0.4%), sepsis (0.4%), increased AST (0.3%), drug hypersensitivity (0.3%), fatigue (0.3%), and thrombocytopenia (0.3%).

Dosage interruptions due to an adverse reaction occurred in 42% of patients who received RETEVMO. Adverse reactions requiring dosage interruption in ≥ 2% of patients included ALT increased, AST increased, hypertension, diarrhea, pyrexia, and QT prolongation.

Dose reductions due to an adverse reaction occurred in 31% of patients who received RETEVMO. Adverse reactions requiring dosage reductions in ≥ 2% of patients included ALT increased, AST increased, QT prolongation and fatigue.

The most common adverse reactions, including laboratory abnormalities, (≥ 25%) were increased aspartate aminotransferase (AST), increased alanine aminotransferase (ALT), increased glucose, decreased leukocytes, decreased albumin, decreased calcium, dry mouth, diarrhea, increased creatinine, increased alkaline phosphatase, hypertension, fatigue, edema, decreased platelets, increased total cholesterol, rash, decreased sodium, and constipation.

Table 5 summarizes the adverse reactions in LIBRETTO-001.

Table 5 : Adverse Reactions (≥ 15%) in Patients Who Received RETEVMO in LIBRETTO-001

Adverse ReactionRETEVMO
(n = 702)
Grades 1-4 (%)Grades 3-4 (%)
Gastrointestinal
Dry Mouth390
Diarrhea1373.4*
Constipation250.6*
Nausea230.6*
Abdominal pain2231.9*
Vomiting150.3*
Vascular
Hypertension3518
General
Fatigue3352*
Edema4330.3*
Skin
Rash5270.7*
Nervous System
Headache6231.4*
Respiratory
Cough7180
Dyspnea8162.3
Investigations
Prolonged QT interval174*
Blood and Lymphatic System
Hemorrhage9151.9
1Diarrhea includes diarrhea, defecation urgency, frequent bowel movements, and anal incontinence
2Abdominal pain includes abdominal pain, abdominal pain upper, abdominal pain lower, abdominal discomfort, gastrointestinal pain
3Fatigue includes fatigue, asthenia, malaise.
4Edema includes edema, edema peripheral, face edema, eye edema, eyelid edema, generalized edema, localized edema, lymph edema, scrotal edema, peripheral swelling, scrotal swelling, swelling, swelling face, eye swelling, peripheral swelling
5Includes rash, rash erythematous, rash macular, rash maculopapular, rash morbilliform, rash pruritic
6Headache includes headache, sinus headache, tension headache
7Includes cough, productive cough
8Includes dyspnea, dyspnea exertional, dyspnea at rest
9Hemorrhage includes epistaxis, hematuria, hemoptysis, contusion, rectal hemorrhage, vaginal hemorrhage, ecchymosis, hematochezia, petechiae, traumatic hematoma, anal hemorrhage, blood blister, blood urine present, cerebral hemorrhage, gastric hemorrhage, hemorrhage intracranial, spontaneous hematoma, abdominal wall hematoma, angina bullosa hemorrhagica, diverticulum intestinal hemorrhagic, eye hemorrhage, gastrointestinal hemorrhage, gingival bleeding, hematemesis, hemorrhagic anemia, intraabdominal hemorrhage, lower gastrointestinal hemorrhage, melena, mouth hemorrhage, occult blood positive, pelvic hematoma, periorbital hematoma, pharyngeal hemorrhage, pulmonary contusion, purpura, retroperitoneal hematoma, subarachnoid hemorrhage, subdural hemorrhage, upper gastrointestinal hemorrhage, vessel puncture site hematoma
*Only includes a grade 3 adverse reaction.

Clinically relevant adverse reactions in ≤ 15% of patients who received RETEVMO include hypothyroidism (9%).

Table 6 summarizes the laboratory abnormalities in LIBRETTO-001.

Table 6 : Select Laboratory Abnormalities (≥ 20%) Worsening from Baseline in Patients Who Received RETEVMO in LIBRETTO-001

Laboratory AbnormalityRETEVMO1
Grades 1-4 (%)Grades 3-4 (%)
Chemistry
Increased AST518
Increased ALT459
Increased glucose442.2
Decreased albumin420.7
Decreased calcium413.8
Increased creatinine371.0
Increased alkaline phosphatase362.3
Increased total cholesterol310.1
Decreased sodium277
Decreased magnesium240.6
Increased potassium241.2
Increased bilirubin232.0
Decreased glucose220.7
Hematology
Decreased leukocytes431.6
Decreased platelets332.7
1 Denominator for each laboratory parameter is based on the number of patients with a baseline and post-treatment laboratory value available, which ranged from 675 to 692 patients.

Increased Creatinine

In healthy subjects administered RETEVMO 160 mg orally twice daily, serum creatinine increased 18% after 10 days. Consider alternative markers of renal function if persistent elevations in serum creatinine are observed [see CLINICAL PHARMACOLOGY].

Read the entire FDA prescribing information for Retevmo (Selpercatinib Capsules)

Related Resources for Retevmo

© Retevmo Patient Information is supplied by Cerner Multum, Inc. and Retevmo Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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