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Retevmo was evaluated in a phase I/II trial: the largest trial ever reported in patients with RET-driven cancer1

702 patients with certain RET-altered advanced solid tumors were included in LIBRETTO-001, an open-label, single-arm, multicenter, phase I/II, multicohort trial.1-3*

LIBRETTO-001 Trial Design

Phase 1 dose escalation: Retevmo dosed at 20 mg QD–240 mg BID. Intra-patient dose escalation was allowed by protocol.4
Phase 2 dose: Retevmo dosed at 160 mg BID.4

See full Prescribing Information for dosing instructions.

Objective response rate (ORR) was defined as complete response (CR) + partial response (PR) and was assessed by independent review committee (IRC) according to Response Evaluation Criteria in Solid Tumors (RECIST) v1.1.1

The intent-to-treat (ITT) population was analyzed in the LIBRETTO-001 trial because this type of analysis avoids the selective exclusion of patients, which can lead to a biased assessment of an intervention's effectiveness.5-8

*Patients with RET-mutant NSCLC and RET-mutant thyroid cancer (non-medullary thyroid cancer (non-MTC)) were not enrolled in the trial since RET is not the driver of tumor growth in these cancers.1,9
†Patients with advanced or metastatic RET fusion-positive NSCLC who had progressed on platinum-based chemotherapy and those without prior systemic therapy were enrolled in separate cohorts.1
‡Non-medullary thyroid cancers (non-MTC) by histology included papillary (n=31), poorly differentiated (n=4), anaplastic (n=2), and Hurthle cell (n=1).1,3
§Other tumors included pancreatic cancer (n=7), colon cancer (n=5), and adrenal gland carcinoma (n=3).3
‖Number of patients included in the initial efficacy analysis. Efficacy was based on patients who had at least 6 months of follow-up.1
¶Efficacy was evaluated in 105 adult patients with metastatic RET fusion-positive NSCLC who were previously treated with platinum chemotherapy enrolled into a cohort of LIBRETTO-001. All 105 patients received systemic therapy (with a median of 3 prior systemic regimens). 58 of the 105 patients received prior anti-PD-1/PD-L1 therapy, and 50 of the 105 patients received a prior multikinase inhibitor (MKI).1,3
#Patients in this cohort received no prior systemic therapy other than radioactive iodine (RAI).1
**Patients in this cohort received a prior systemic therapy (including sorafenib, lenvatinib, or both) other than RAI.1
††The efficacy of Retevmo was evaluated in 55 patients with RET-mutant advanced MTC who were previously treated with cabozantinib or vandetanib enrolled into a cohort of LIBRETTO-001.1

BID=twice daily; CNS=central nervous system; DoR=duration of response; MTC=medullary thyroid cancer; NSCLC=non-small cell lung cancer; OS=overall survival; PFS=progression-free survival; QD=once daily; RET=rearranged during transfection.

See efficacy results in patients with certain RET-driven NSCLC and thyroid cancer

Response in patients with metastatic RET fusion-positive NSCLC1

Treatment-naive patients (n=39)1,10

85% objective response rate ORR for treatment-naïve patients with metastatic RET fusion-positive NSCLC


Median DoR not yet reached

(95% CI: 12, NE)
Median follow-up: 7.4 months1,11

The major efficacy outcome measures in LIBRETTO-001 were objective response rate (ORR) and duration of response (DoR). Disease control rate (DCR) was not a prespecified endpoint and is a post-hoc calculation. DCR is defined as ORR (CR + PR) + SD.

Stable disease (SD) is defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for progressive disease (PD), per Response Evaluation Criteria in Solid Tumors (RECIST) v1.1. In the setting of a single-arm trial without the ability to compare with a control arm provided by a randomized trial, the interpretation and clinical relevance of a best overall response of SD are not clear, and it is not possible to determine if SD is a result of natural disease progression or treatment with Retevmo.1,12

For treatment-naive patients who responded (n=33) to treatment, the median time to objective response was 1.8 months (range: 0.7, 3.7)13‡‡

Time to any and best response was a prespecified secondary endpoint.13

Time-to-event endpoints are not interpretable in a single-arm study.



Previously treated§§ patients (n=105)1,10

64% objective response rate ORR for previously treated* patients with metastatic RET fusion-positive NSCLC


Median DoR

17.5

months

(95% CI: 12, NE)
Median follow-up: 12.1 months1,11

For previously treated§§ patients who responded (n=67) to treatment, the median time to objective response was 1.9 months (range: 0.7, 13.7)13‡‡

Time to any and best response was a prespecified secondary endpoint.13

Time-to-event endpoints are not interpretable in a single-arm study.


All results reviewed by an IRC.1,10,11,13

Due to rounding, numbers presented may not add up to the totals indicated and percentages may not reflect the absolute figures for the same reason.

‡‡According to the protocol, scans were to be performed every 8 weeks (±7 days). The protocol allowed investigators to conduct an initial scan at 4 weeks (±7 days).14
§§Efficacy was evaluated in 105 adult patients with metastatic RET fusion-positive NSCLC who were previously treated with platinum chemotherapy enrolled into a cohort of LIBRETTO-001. All 105 patients received systemic therapy (with a median of 3 prior systemic regimens).1

Retevmo has CNS activity in patients with measurable brain metastases (n=11). CNS ORR was observed in the LIBRETTO-001 trial1‖‖

No patients received radiation therapy (RT) to the brain within 2 months prior to study entry.1

Responses in intracranial lesions were observed in 10 of 11 previously treated patients with measurable brain metastases

CNS DoR was ≥6 months in all responders with measurable brain metastases1‖‖

‖‖Patients previously treated with platinum-based chemotherapy and with measurable CNS lesions at baseline according to IRC assessment.1

CNS ORR and CNS DoR were prespecified secondary endpoints in the LIBRETTO-001 trial that were evaluated and confirmed by an IRC.1,3

Additional CNS analysis

In a prespecified analysis which included both treatment-naive and treatment-experienced patients with metastatic RET fusion-positive NSCLC, an additional 11 patients with measurable brain metastases were included (n=22). Intracranial responses were seen in 18 of these 22 patients (82% CNS ORR) (95% CI: 60, 95), with a 9.4-month median CNS DoR (95% CI: 7.4, NE) in the LIBRETTO-001 trial.15

The initial CNS data analysis included 11 patients with measurable brain metastases who completed prior RT >2 months prior to Retevmo and were previously treated with platinum-based chemotherapy. An additional CNS analysis included 11 more measurable patients who could have received prior RT ≤2 months of Retevmo; 9 were previously treated with or without platinum-based chemotherapy and 2 were treatment naive. In total, 20 out of 22 were previously treated with: platinum chemotherapy (n=16), anti-PD-1/PD-L1 therapy (n=12), and/or a multi-targeted kinase inhibitor (MKI) (n=11). 8 out of 22 received prior brain RT; 6 of the 8 completed brain RT >2 months prior to Retevmo.1,15


Select Important Safety Information

Hypertension occurred in 35% of patients, including Grade 3 hypertension in 17% and Grade 4 in one (0.1%) patient. Overall, 4.6% 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 dose, or permanently discontinue Retevmo based on the severity.

Response in patients with advanced or metastatic RET fusion-positive thyroid cancer (non-MTC)1¶¶

Systemic therapy-naive## patients (n=8)1,16

100% objective response rate ORR for systemic therapy-naïve patients with advanced or metastatic RET fusion-positive thyroid cancer


Median DoR not yet reached

(95% CI: NE, NE)
Median follow-up: 8.8 months1,11

The major efficacy outcome measures in LIBRETTO-001 were ORR and DoR. DCR was not a prespecified endpoint and is a post-hoc calculation. DCR is defined as ORR (CR + PR) + SD.

SD is defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, per RECIST v1.1. In the setting of a single-arm trial without the ability to compare with a control arm provided by a randomized trial, the interpretation and clinical relevance of a best overall response of SD are not clear, and it is not possible to determine if SD is a result of natural disease progression or treatment with Retevmo.1,12



Previously treated*** patients (n=19)1,16

79% objective response rate ORR for previously treated patients with advanced or metastatic RET fusion-positive thyroid cancer


Median DoR

18.4

months

(95% CI: 7.6, NE)
Median follow-up: 17.5 months1,11

All results reviewed by an IRC.1,11,16

¶¶Primary tumor histologies included papillary thyroid cancer, poorly differentiated thyroid cancer, anaplastic thyroid cancer, and Hurthle cell thyroid cancer.1
##Patients received no prior systemic therapy other than RAI.1
***Patients received a prior systemic therapy (including sorafenib, lenvatinib, or both) other than RAI.1

Response in patients with advanced or metastatic RET-mutant MTC1

Cabozantinib/vandetanib-naive patients (n=88)1,17

69% objective response rate ORR for patients previously treated with cabozantiniband or vandetanib  with advanced or metastatic RET-mutant medullary thyroid cancer


Median DoR

22.0

months

(95% CI: NE, NE)
Median follow-up: 7.8 months1,11

The major efficacy outcome measures in LIBRETTO-001 were ORR and DoR. DCR was not a prespecified endpoint and is a post-hoc calculation. DCR is defined as ORR (CR + PR) + SD.

SD is defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, per RECIST v1.1. In the setting of a single-arm trial without the ability to compare with a control arm provided by a randomized trial, the interpretation and clinical relevance of a best overall response of SD are not clear, and it is not possible to determine if SD is a result of natural disease progression or treatment with Retevmo.1,12



Patients previously treated††† with cabozantinib and/or vandetanib (n=55)1,17

73% objective response rate ORR for cabozantinib/vandetanib treatment-naïve patients with advanced or metastatic RET-mutant medullary thyroid cancer


Median DoR not yet reached

(95% CI: 19.1, NE)
Median follow-up: 14.1 months1,11

All results reviewed by an IRC.1,11,17

†††The efficacy of Retevmo was evaluated in 55 patients with RET-mutant advanced MTC who were previously treated with cabozantinib or vandetanib enrolled into a cohort of LIBRETTO-001.1


Because Retevmo is approved across all lines of therapy, including first line in certain RET-driven cancers, consider waiting for genomic test results, including RET alteration results, before making therapeutic decisions1

An FDA-approved test for the detection of RET gene fusions and RET gene mutations is not currently available for Retevmo.1


Select Important Safety Information

Retevmo can cause concentration-dependent QT interval prolongation. An increase in QTcF interval to >500 ms was measured in 6% of patients and an increase in the QTcF interval of at least 60 ms over baseline was measured in 15% of patients. 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 dose reduce or permanently discontinue Retevmo based on the severity.

National Comprehensive Cancer Network® (NCCN®) NSCLC Panel recommends selpercatinib (Retevmo) as a first-line or subsequent‡‡‡ therapy option for patients with metastatic NSCLC who are positive for RET rearrangements18

NCCN makes no warranties of any kind whatsoever regarding their content, use or application and disclaims any responsibility for their application or use in any way.

NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) recommendations for RET alteration-positive thyroid cancer19:

Selpercatinib is a recommended systemic therapy option (category 2A§§§) in RET fusion-positive:

  • Structurally persistent/recurrent locoregional or distant metastatic (including bone or CNS metastases) papillary carcinoma, follicular carcinoma, or Hurthle carcinoma, that is not amenable to RAI therapy

Selpercatinib is a preferred systemic therapy option (category 2A§§§) in RET fusion-positive:

  • Metastatic anaplastic carcinoma‖‖‖

Selpercatinib is a preferred systemic therapy option (category 2A§§§) in RET mutation-positive medullary carcinoma¶¶¶:

  • Locoregional, unresectable carcinoma that is symptomatic or progressing by RECIST criteria
  • Distant metastatic, asymptomatic carcinoma that is unresectable and progressing by RECIST criteria
  • Distant metastatic, symptomatic or progressive carcinoma

‡‡‡If not previously used.
§§§Category 2A: Based upon lower-level evidence, and there is uniform NCCN consensus that the intervention is appropriate.
ǁǁǁMolecular testing should include BRAF, NTRK, ALK, RET, and tumor mutational burden.
¶¶¶RET somatic genotyping in patients who are germline wild-type or germline unknown.

See NCCN Guidelines® recommendations for RET testing
See safety results for Retevmo

CI=confidence interval; NE=not estimable.

References: 1. Retevmo (selpercatinib) [package insert]. Indianapolis, IN: Eli Lilly and Company; 2020. 2. Phase 1/2 study of LOXO-292 in patients with advanced solid tumors, RET fusion-positive solid tumors, and medullary thyroid cancer (LIBRETTO-001). https://clinicaltrials.gov/ct2/show/NCT03157128. Updated July 2, 2020. Accessed July 16, 2020. 3. Data on File, Lilly USA, LLC, DOF-SE-US-0033. 4. Drilon A, Oxnard G, Wirth L, et al. Registrational results of LIBRETTO-001: a phase 1/2 trial of selpercatinib (LOXO-292) in patients with RET fusion-positive lung cancers. Presented at: 2019 World Conference on Lung Cancer; September 7–10, 2019; Barcelona, Spain. 5. Drilon A, Oxnard GR, Tan DSW, et al. Efficacy of selpercatinib in RET fusion–positive non–small-cell lung cancer. N Engl J Med. 2020;383(9):813-824. 6. Wirth LJ, Sherman E, Robinson B, et al. Efficacy of selpercatinib in RET-altered thyroid cancers. N Engl J Med. 2020;383(9):825-835. 7. McCoy CE. Understanding the intention-to-treat principle in randomized controlled trials. West J Emerg Med. 2017;18(6):1075-1078. 8. Gupta SK. Intention-to-treat concept: a review. Perspect Clin Res. 2011;2(3):109-112. 9. Mulligan LM. GDNF and the RET receptor in cancer: new insights and therapeutic potential. Front Physiol. 2019;9:1873. 10. Data on File, Lilly USA, LLC, DOF-SE-US-0023. 11. Data on File, Lilly USA, LLC, DOF-SE-US-0032. 12. Villaruz LC, Socinski MA. The clinical viewpoint: definitions, limitations of RECIST, practical considerations of measurement. Clin Cancer Res. 2013;19(10):2629-2636. 13. Data on File, Lilly USA, LLC, DOF-SE-US-0028. 14. Data on File, Lilly USA, LLC, DOF-SE-US-0013. 15. Subbiah V, Gainor JF, Oxnard GR, et al. Intracranial activity of selpercatinib (LOXO-292) in RET fusion-positive non-small cell lung cancer (NSCLC) patients on the LIBRETTO-001 trial. Poster presented at: 2020 ASCO Annual Meeting; May 29–June 2, 2020; Virtual Meeting. Abstract 9516. 16. Data on File, Lilly USA, LLC, DOF-SE-US-0031. 17. Data on File, Lilly USA, LLC, DOF-SE-US-0024. 18. Referenced with permission from The NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for Non-Small Cell Lung Cancer V.8.2020. © National Comprehensive Cancer Network, Inc. 2020. All rights reserved. Accessed September 15, 2020. To view the most recent and complete version of the guidelines, go online to https://www.nccn.org. 19. Referenced with permission from The NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for Thyroid Carcinoma V.2.2020. © National Comprehensive Cancer Network, Inc. 2020. All rights reserved. Accessed July 15, 2020. To view the most recent and complete version of the guidelines, go online to https://www.nccn.org.

Indications

Retevmo is a kinase inhibitor indicated for the treatment of:

  • 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
  • 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)

These indications are approved under accelerated approval based on overall response rate (ORR) and duration of response (DoR). Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials.

Important Safety Information for Retevmo® (selpercatinib)

Hepatotoxicity: Serious hepatic adverse reactions occurred in 2.6% of patients treated with Retevmo. Increased aspartate aminotransferase (AST) occurred in 51% of patients, including Grade 3 or 4 events in 8% and increased alanine aminotransferase (ALT) occurred in 45% of patients, including Grade 3 or 4 events in 9%. The median time to first onset for increased AST was 4.1 weeks (range: 5 days to 2 years) and increased ALT was 4.1 weeks (range: 6 days to 1.5 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 dose or permanently discontinue Retevmo based on the severity.

Hypertension occurred in 35% of patients, including Grade 3 hypertension in 17% and Grade 4 in one (0.1%) patient. Overall, 4.6% 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 dose, or permanently discontinue Retevmo based on the severity.

Retevmo can cause concentration-dependent QT interval prolongation. An increase in QTcF interval to >500 ms was measured in 6% of patients and an increase in the QTcF interval of at least 60 ms over baseline was measured in 15% of patients. 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 dose reduce or permanently discontinue Retevmo based on the severity.

Serious, including fatal, hemorrhagic events can occur with Retevmo. Grade ≥3 hemorrhagic events occurred in 2.3% of patients treated with Retevmo including 3 (0.4%) patients with fatal hemorrhagic events, including one case each of cerebral hemorrhage, tracheostomy site hemorrhage, and hemoptysis. Permanently discontinue Retevmo in patients with severe or life-threatening hemorrhage.

Hypersensitivity occurred in 4.3% of patients receiving Retevmo, including Grade 3 hypersensitivity in 1.6%. The median time to onset was 1.7 weeks (range 6 days to 1.5 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. 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. Continue steroids until patient reaches target dose and then taper. Permanently discontinue Retevmo for recurrent hypersensitivity.

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.

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 of the potential risk to a fetus. Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during treatment with Retevmo and for at least 1 week after the final dose. 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 final dose.

Severe adverse reactions (Grade 3-4) occurring in ≥15% of patients who received Retevmo in LIBRETTO-001, were hypertension (18%), prolonged QT interval (4%), diarrhea (3.4%), dyspnea (2.3%), fatigue (2%), abdominal pain (1.9%), hemorrhage (1.9%), headache (1.4%), rash (0.7%), constipation (0.6%), nausea (0.6%), vomiting (0.3%), and edema (0.3%).

Serious adverse reactions occurred in 33% of patients who received Retevmo. The most frequently reported 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).

Common adverse reactions (all grades) occurring in ≥15% of patients who received Retevmo in LIBRETTO-001, were dry mouth (39%), diarrhea (37%), hypertension (35%), fatigue (35%), edema (33%), rash (27%), constipation (25%), nausea (23%), abdominal pain (23%), headache (23%), cough (18%), prolonged QT interval (17%), dyspnea (16%), vomiting (15%), and hemorrhage (15%).

Laboratory abnormalities (all grades; Grade 3-4) ≥20% worsening from baseline in patients who received Retevmo in LIBRETTO-001, were AST increased (51%; 8%), ALT increased (45%; 9%), increased glucose (44%; 2.2%), decreased leukocytes (43%; 1.6%), decreased albumin (42%; 0.7%), decreased calcium (41%; 3.8%), increased creatinine (37%; 1.0%), increased alkaline phosphatase (36%; 2.3%), decreased platelets (33%; 2.7%), increased total cholesterol (31%; 0.1%), decreased sodium (27%; 7%), decreased magnesium (24%; 0.6%), increased potassium (24%; 1.2%), increased bilirubin (23%; 2.0%), and decreased glucose (22%; 0.7%).

Concomitant use of acid-reducing agents decreases selpercatinib plasma concentrations which may reduce Retevmo anti-tumor activity. Avoid concomitant use of proton-pump inhibitors (PPIs), histamine-2 (H2) receptor antagonists, and locally-acting antacids with Retevmo. If coadministration cannot be avoided, take Retevmo with food (with a PPI) or modify its administration time (with a H2 receptor antagonist or a locally-acting antacid).

Concomitant use of strong and moderate CYP3A inhibitors increases selpercatinib plasma concentrations which may increase the risk of Retevmo adverse reactions including QTc interval prolongation. 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 dosage as recommended and monitor the QT interval with ECGs more frequently.

Concomitant use of strong and moderate CYP3A inducers decreases selpercatinib plasma concentrations which may reduce Retevmo anti-tumor activity. Avoid coadministration of Retevmo with strong and moderate CYP3A inducers.

Concomitant use of Retevmo with CYP2C8 and CYP3A substrates increases their plasma concentrations which may increase the risk of adverse reactions related to these substrates. Avoid coadministration of Retevmo with CYP2C8 and CYP3A substrates where minimal concentration changes may lead to increased adverse reactions. If coadministration cannot be avoided, follow recommendations for CYP2C8 and CYP3A substrates provided in their approved product labeling.

The safety and effectiveness of Retevmo have not been established in pediatric patients less than 12 years of age. 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). Use of Retevmo for these indications is supported by evidence from adequate and well-controlled studies in adults with additional pharmacokinetic and safety data in pediatric patients aged 12 years and older.

No dosage modification is recommended for patients with mild to moderate renal impairment (creatinine clearance [CLcr] ≥30 mL/Min, estimated by Cockcroft-Gault). A recommended dosage has not been established for patients with severe renal impairment or end-stage renal disease.

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

Please see full Prescribing Information for Retevmo.

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