Exkivity

Medical Editor: John P. Cunha, DO, FACOEP Last updated on RxList: 9/22/2021
Exkivity Side Effects Center

What Is Exkivity?

Exkivity (mobocertinib) is a kinase inhibitor used to treat adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after platinum-based chemotherapy.

What Are Side Effects of Exkivity?

Side effects of Exkivity include:

Dosage for Exkivity

The recommended dosage of Exkivity is 160 mg orally once daily, with or without food.

Exkivity In Children

The safety and effectiveness of Exkivity in pediatric patients have not been established.

What Drugs, Substances, or Supplements Interact with Exkivity?

Exkivity may interact with other medicines such as:

  • strong or moderate CYP3A inhibitors,
  • strong or moderate CYP3A inducers,
  • hormonal contraceptives,
  • other CYP3A substrates, and
  • other medications known to prolong the QTc interval

Tell your doctor all medications and supplements you use.

Exkivity During Pregnancy and Breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant before using Exkivity; it may harm a fetus. The pregnancy status in females of reproductive potential should be verified prior to initiating Exkivity. Females of reproductive potential and males with female partners of reproductive potential are advised to use effective non-hormonal contraception during treatment with Exkivity and for 1 month after the last dose. Exkivity may render hormonal contraceptives ineffective. Because of the potential for serious adverse reactions in breastfed children, breastfeeding is not recommended while using Exkivity and for 1 week after the last dose.

Additional Information

Our Exkivity (mobocertinib) 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.

SLIDESHOW

Lung Cancer: Early Signs, Symptoms, Stages See Slideshow
Exkivity Professional Information

SIDE EFFECTS

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

  • QTc Prolongation and Torsades de Pointes [see WARNINGS AND PRECAUTIONS]
  • Interstitial Lung Disease (ILD)/Pneumonitis [see WARNINGS AND PRECAUTIONS]
  • Cardiac Toxicity [see WARNINGS AND PRECAUTIONS]
  • Diarrhea [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.

The pooled safety population described in WARNINGS AND PRECAUTIONS reflects exposure to EXKIVITY as a single agent at a dose of 160 mg orally once daily in 256 patients, including 114 patients with EGFR exon 20 insertion mutation-positive locally advanced or metastatic NSCLC from Study AP32788-15-101, and patients with other solid tumors. Forty-eight percent (48%) were exposed for 6 months or longer and 12% were exposed for greater than one year. The most common (>20%) adverse reactions were diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, and musculoskeletal pain. The most common (≥2%) Grade 3 or 4 laboratory abnormalities were decreased lymphocytes, increased amylase, increased lipase, decreased potassium, decreased hemoglobin, increased creatinine, and decreased magnesium.

EGFR Exon 20 Insertion Mutation-Positive Locally Advanced Or Metastatic NSCLC Previously Treated With Platinum-Based Chemotherapy

The safety of EXKIVITY was evaluated in a subset of patients in Study AP32788-15-101 with EGFR exon 20 insertion mutation-positive locally advanced or metastatic NSCLC who received prior platinum-based chemotherapy [see Clinical Studies]. Patients with a history of interstitial lung disease, drug-related pneumonitis, radiation pneumonitis that required steroid treatment; significant, uncontrolled, active cardiovascular disease; or prolonged QTc interval were excluded from enrollment in this trial. A total of 114 patients received EXKIVITY 160 mg once daily until disease progression or unacceptable toxicity; 60% were exposed for 6 months or longer and 14% were exposed for greater than 1 year.

Serious adverse reactions occurred in 46% of patients who received EXKIVITY. Serious adverse reactions in ≥2% of patients included diarrhea, dyspnea, vomiting, pyrexia, acute kidney injury, nausea, pleural effusion, and cardiac failure. Fatal adverse reactions occurred in 1.8% of patients who received EXKIVITY, including cardiac failure (0.9%), and pneumonitis (0.9%).

Permanent discontinuation occurred in 17% of patients who received EXKIVITY. Adverse reactions requiring permanent discontinuation of EXKIVITY in at least ≥2% of patients were diarrhea and nausea.

Dosage interruptions of EXKIVITY due to an adverse reaction occurred in 51% of patients. Adverse reactions which required dosage interruption in >5% of patients included diarrhea, nausea and vomiting.

Dose reductions of EXKIVITY due to an adverse reaction occurred in 25% of patients. The adverse reaction requiring dose reduction in >5% of patients was diarrhea.

Table 3 summarizes the adverse reactions in Study AP32788-15-101.

Table 3: Adverse Reactions (≥10%) in Patients with EGFR Exon 20 Insertion Mutation-Positive NSCLC Whose Disease Has Progressed on or after Platinum-Based Chemotherapy in Study AP32788-15-101

Adverse Reaction EXKIVITY
(N = 114)
All Grades* (%) Grade 3 or 4 (%)
Gastrointestinal Disorders
Diarrhea 92 22
Stomatitisa 46 4.4**
Vomiting 40 2.6**
Decreased appetite 39 0.9**
Nausea 37 4.4**
Decreased weight 21 0
Abdominal painb 18 1.8**
Gastroesophageal reflux disease 15 0
Dyspepsia 11 0
Skin and Subcutaneous Tissue Disorders
Rashc 78 1.8**
Paronychiad 39 0.9**
Dry skin 32 0
Pruritus 24 0.9**
Alopecia 19 0
Musculoskeletal and Connective Tissue Disorders
Musculoskeletal paine 34 2.6**
General Disorders and Administration Site Conditions
Fatiguef 29 3.5**
Respiratory, Thoracic and Mediastinal Disorders
Coughg 24 0
Upper respiratory tract infectionh 16 0
Dyspneai 15 4.4
Rhinorrhea 13 0
Eye Disorders
Ocular Toxicityj 11 0
Cardiac Disorders
QTc interval prolongationk 10 3.5
Hypertensionl 10 4.4**
Nervous System Disorders
Headache 10 0
* Graded according to National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE 5) ** Events of Grade 3 only (no Grade 4 occurred)
a Stomatitis includes angular cheilitis, aphthous ulcer, cheilitis, mouth ulceration, mucosal inflammation, odynophagia, and stomatitis.
b Abdominal pain includes abdominal discomfort, abdominal pain, abdominal pain upper, abdominal tenderness, and gastrointestinal pain.
c Rash includes acne, dermatitis, dermatitis acneiform, rash, rash macular, rash maculo-papular, rash papular, rash pruritic, rash pustular, and urticaria.
d Paronychia includes nail bed tenderness, nail disorder, nail infection, onycholysis, and paronychia.
e Musculoskeletal pain includes arthralgia, back pain, musculoskeletal chest pain, musculoskeletal discomfort, musculoskeletal pain, myalgia, neck pain, non-cardiac chest pain, pain in extremity, and spinal pain.
f Fatigue includes asthenia, and fatigue.
g Cough includes cough, productive cough, and upper-airway cough syndrome.
h Upper respiratory tract infection includes nasopharyngitis, pharyngitis, respiratory tract infection, rhinitis, sinusitis, and upper respiratory tract infection.
i Dyspnea includes dyspnea, and dyspnea exertional.
j Ocular toxicity includes dry eye, eye pruritis, abnormal sensation in eye, eye discharge, blepharitis, trichiasis, conjunctival hemorrhage, vitreous floaters, blurred vision and corneal edema.
k QTc interval prolongation includes electrocardiogram QT prolonged, and ventricular arrhythmia.
l Hypertension includes blood pressure increased, and hypertension.

Clinically relevant adverse reactions in <10% of patients receiving EXKIVITY included edema (9%), acute kidney injury (8%), peripheral neuropathy (7%), palmar-plantar erythrodysaesthesia (4.4%), pneumonitis (2.6%) and cardiac failure (2.6%).

Table 4 summarizes the laboratory abnormalities in Study AP32788-15-101.

Table 4: Select Laboratory Abnormalities (≥20%) Worsening from Baseline in Patients with EGFR Exon 20 Insertion Mutation-Positive NSCLC Whose Disease Has Progressed on or after Platinum-Based Chemotherapy in Study AP32788-15-101

Laboratory Abnormality EXKIVITY**
(N = 114)
All Grades* (%) Grade 3 or 4 (%)
Hematology
Decreased red blood cells 59 3.5
Decreased lymphocytes 52 15
Decreased platelets 26 0.9
Decreased leukocytes 25 0
Chemistry
Increased creatinine 52 2.7
Increased amylase 40 13
Increased lipase 35 10
Decreased potassium 29 5.3
Increased alkaline phosphatase 25 1.8
Decreased albumin 23 1.8
Decreased magnesium 23 2.7
Increased alanine aminotransferase 22 2.7
Increased aspartate aminotransferase 21 1.8
Decreased sodium 20 0.9
* Grades per NCI CTCAE v5.0
** The denominator used to calculate the rate varied from 93 to 113 based on the number of patients with a baseline and at least one post-treatment value. The laboratory abnormalities are values that reflect worsening from baseline.

DRUG INTERACTIONS

Effect Of Other Drugs On EXKIVITY

Strong or Moderate CYP3A Inhibitors
Clinical Impact
  • Coadministration of EXKIVITY with strong or moderate CYP3A inhibitors increased mobocertinib plasma concentrations [see CLINICAL PHARMACOLOGY], which may increase the risk of adverse reactions, including QTc interval prolongation.
Prevention or Management
  • Avoid concomitant use of strong or moderate CYP3A inhibitors with EXKIVITY. If concomitant use of moderate CYP3A inhibitors cannot be avoided, reduce the EXKIVITY dose and monitor the QTc interval more frequently with ECGs [see DOSAGE AND ADMINISTRATION, WARNINGS AND PRECAUTIONS].
Strong or Moderate CYP3A Inducers
Clinical Impact
  • Coadministration of EXKIVITY with strong or moderate CYP3A inducers decreased mobocertinib plasma concentrations [see CLINICAL PHARMACOLOGY], which may reduce EXKIVITY anti-tumor activity.
Prevention or Management
  • Avoid concomitant use of strong or moderate CYP3A inducers with EXKIVITY.

Effect Of EXKIVITY On Other Drugs

CYP3A Substrates
Clinical Impact
  • Coadministration of EXKIVITY with CYP3A substrates may decrease plasma concentrations of CYP3A substrates [see CLINICAL PHARMACOLOGY], which may reduce the efficacy of these substrates.
Prevention or Management
  • Avoid concomitant use of hormonal contraceptives with EXKIVITY [see WARNINGS AND PRECAUTIONS, Use In Specific Populations (8.3)].
  • Avoid concomitant use of EXKIVITY with other CYP3A substrates where minimal concentration changes may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with the approved product Prescribing Information.

Drugs That Prolong The QTc Interval

Clinical Impact
  • EXKIVITY can cause QTc interval prolongation [see WARNINGS AND PRECAUTIONS, CLINICAL PHARMACOLOGY]. Coadministration of EXKIVITY with drugs known to prolong the QTc interval may increase the risk of QTc interval prolongation [see WARNINGS AND PRECAUTIONS, CLINICAL PHARMACOLOGY].
Prevention or Management
  • Avoid concomitant use of other medications known to prolong the QTc interval with EXKIVITY. If concomitant use is unavoidable, monitor the QTc interval more frequently with ECGs [seeWARNINGS AND PRECAUTIONS].

Read the entire FDA prescribing information for Exkivity (Mobocertinib Capsules)

QUESTION

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

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

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