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Retevmo ® (selpercatinib) tablets

40 mg, 80 mg, 120 mg, 160 mg

Full Prescribing Information

This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.

Is Retevmo® (selpercatinib) safe and effective in thyroid cancer?

In LIBRETTO clinical trials, selpercatinib demonstrated durable antitumor activity, with a tolerable safety profile in patients with RET-altered thyroid cancer.

US_cFAQ_SEL202_X2_USE_IN_THYROID
US_cFAQ_SEL202_X2_USE_IN_THYROIDen-US

Use of Selpercatinib in Thyroid Cancer

LIBRETTO-531

Efficacy of Selpercatinib in RET-Mutant Medullary Thyroid Cancer

At the interim analysis, LIBRETTO-531 met the criteria for positive progression-free survival (PFS) and treatment failure-free survival (TFFS). At a median follow-up of approximately 12 months, the blinded independent central review (BICR)-assessed median PFS in the selpercatinib arm was not reached and the BICR-assessed median PFS in the control arm was 16.8 months. This corresponds to a hazard ratio (HR) of 0.280 (95% CI, 0.164 - 0.475; p<0.0001), which indicates a significant improvement in PFS with selpercatinib. Also, selpercatinib improved TFFS (HR: 0.254, 95% CI, 0.153 - 0.423; p<0.0001). The overall response rate (ORR) by BICR was 69.4% (95% CI, 62.4 - 75.8) with selpercatinib versus 38.8% (95% CI, 29.1 - 49.2) in the control arm (odds ratio: 3.7, 95% CI, 2.2 - 6.3; p<0.0001). The observed overall survival (OS) HR was 0.374 (95% CI, 0.147 - 0.949).1

Summary of Outcomes in LIBRETTO-531 by Blinded Independent Central Review1

Outcome Measurea

Selpercatinib

(N=193)

Cabozantinib or Vandetanib

(N=98)

PFS, months (95% CI)

Median 

NE (NE, NE)

16.8 (12.2, 25.1)

Median duration of follow-up

12.5 (11.1, 13.8) 

11.0 (7.7, 16.6)

TFFSb, months (95% CI)

Median

NE (NE, NE)

13.9 (11.3, 25.1)

Median duration of follow-up

12.5 (11.1, 13.8)

11.1 (8.1,16.6)

ORR, % (95% CI) 

69.4 (62.4, 75.8)

38.8 (29.1, 49.2)

Best overall response, n (%)

Complete response

23 (11.9) 

4 (4.1)

Partial response

111 (57.5) 

34 (34.7)

Stable disease

39 (20.2)

48 (49.0)

Progressive disease

4 (2.1) 

1 (1.0)

Not evaluable

16 (8.3) 

11 (11.2)

Abbreviations: CI = confidence interval; NE = not estimable; ORR = overall response rate; PFS = progression-free survival; TFFS = treatment failure-free survival.

aEfficacy measures were assessed by a blinded independent central review.

bTreatment failure-free survival is the time to disease progression, discontinuation due to related adverse event, or death, whichever occurs first (or otherwise censored).

Efficacy by RET Mutation in Patients With RET-Mutant MTC in LIBRETTO-531

A sub-analysis of patients from LIBRETTO-531 treated with selpercatinib versus cabozantinib/vandetanib was conducted​ to investigate the efficacy of selpercatinib by RET mutation in patients with RET-mutant medullary thyroid cancer (MTC). Selpercatinib consistently outperformed the control across all RET mutation groups. Across M918T, extracellular cysteine, and other RET mutation groups, selpercatinib demonstrated similar robust and durable responses, consistent with previously reported efficacy of selpercatinib for patients with RET-mutant MTC.2 

Safety of Selpercatinib in RET-Mutant Medullary Thyroid Cancer

Adverse events were consistent with those previously reported for selpercatinib and the control regimen. Treatment-emergent Adverse Events of Any Grade in ≥20% of Patients in LIBRETTO-531 summarizes the most common treatment-emergent adverse events (TEAEs) occurring in ≥20% of the LIBRETTO-531 safety population.1

Treatment-emergent Adverse Events of Any Grade in ≥20% of Patients in LIBRETTO-5311

 

Selpercatinib

(N = 193)


Cabozantinib or Vandetanib

(N = 97)

TEAE, n (%)

Any Grade

Grade ≥3

Any Grade

Grade ≥ 3

Hypertension

82 (42.5)

36 (18.7)

40 (41.2)

17 (17.5)

Diarrhea 

51 (26.4)

6 (3.1) 

59 (60.8)

8 (8.2)

ALT increased 

51 (26.4)

20 (10.4) 

33 (34.0)

2 (2.1)

AST increased

46 (23.8) 

9 (4.7)

37 (38.1)

2 (2.1)

Dry mouth

61 (31.6)

1 (0.5)

10 (10.3)

1 (1.0)

Headache

44 (22.8) 

1 (0.5)

20 (20.6)

0

Fatigue

36 (18.7) 

7 (3.6) 

21 (21.6)

5 (5.2)

Nausea

20 (10.4) 

2 (1.0)

31 (32.0)

5 (5.2)

Decreased appetite

23 (11.9) 

1 (0.5) 

27 (27.8)

5 (5.2)

Rash

28 (14.5) 

2 (1.0)

20 (20.6)

2 (2.1)

Palmar-plantar erythrodysesthesia syndrome 

6 (3.1) 

0

41 (42.3)

9 (9.3)

Asthenia

21 (10.9) 

1 (0.5) 

24 (24.7)

4 (4.1)

Hypocalcemia

20 (10.4) 

2 (1.0) 

25 (25.8)

7 (7.2)

Mucosal inflammation

14 (7.3)

1 (0.5)

25 (25.8)

13 (13.4)

Weight decreased

10 (5.2)

1 (0.5)

27 (27.8)

4 (4.1)

Vomiting

15 (7.8) 

0

20 (20.6)

2 (2.1)

Proteinuria

3 (1.6) 

0

23 (23.7)

0

Abbreviations: ALT = alanine aminotransferase; AST = aspartate aminotransferase; TEAE = treatment-emergent adverse event.

Compared to patients in the control arm, selpercatinib-treated patients reported less adverse events that led to dose reductions (38.9% vs 77.3%) and drug discontinuation due to an adverse event (4.7% vs 26.8%).1

As of the data cutoff date of May 22, 2023, treatment-emergent AEs leading to death that occurred on study or within 30 days of treatment discontinuation were observed in 2 patients (2.1%) in the control treatment arm who died from AEs of cholangitis and hemorrhage (1 patient each), while in the selpercatinib treatment arm, 4 patients (2.1%) died due to 

  • COVID-19 (n=1)
  • diabetic ketoacidosis (n=1) 
  • multiple organ dysfunction (n=1), and
  • sudden death (n=1).1

The patient with sudden death was considered potentially related to study treatment by the investigator.1

Baseline Characteristics of Patients With RET-Mutant Medullary Thyroid Cancer in LIBRETTO-531

The majority of patients were white, male, and <65 years old. Most rearranged during transfection (RET) mutations were identified by next-generation sequencing (90.4%), and the most common RET mutation was M918T. Patient Baseline Characteristics for LIBRETTO-531 provides detailed information regarding patient baseline characteristics.1

Patient Baseline Characteristics for LIBRETTO-5311

Characteristic

Selpercatinib

(N=193)

Cabozantinib or Vandetanib

(N=98)

Age, years, median (range)

56.0 (12-79)

53.5 (18-84)

Sex, n (%)

Male

115 (59.6)

68 (69.4)

Female

78 (40.4) 

30 (30.6)

Race, n (%)

White

116 (70.7)

52 (66.7)

Asian

43 (26.2)

24 (30.8)

Black

5 (3.0)

2 (2.6)

RET mutation, n (%)

M918T mutation

121 (62.7) 

61 (62.2)

Other mutations

72 (37.3) 

37 (37.8)

Abbreviation: RET = rearranged during transfection.

LIBRETTO-531 Phase 3 Selpercatinib Use in RET-Mutant Medullary Thyroid Cancer

LIBRETTO-531 is a multicenter, randomized, open-label, phase 3 trial comparing selpercatinib to physician's choice of cabozantinib or vandetanib in patients with metastatic, advanced, kinase inhibitor naïve, RET-mutant MTC (NCT04211337). LIBRETTO-531 is currently active.3,4

The primary endpoint was PFS by BICR per Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1.1

Between February 2020 and March 2023, a total of 291 patients with progressive RET-mutant MTC were enrolled at 176 centers across 19 countries. Of the 291 patients, 193 patients were randomly assigned to selpercatinib and 98 patients to the cabozantinib/vandetanib control arm. Patients randomized to the control arm who experienced disease progression confirmed by BICR were eligible to cross over to selpercatinib.1

LIBRETTO-001

Efficacy of Seplercatinib in RET Fusion-Positive Thyroid Cancer

In the January 2023 data cutoff of the phase 1/2 LIBRETTO-001 trial, patients with RET fusion-positive thyroid cancer

  • who were treatment-naïve (N=24), had an objective response rate (ORR) of 95.8% with a median duration of response (DOR) that was not estimable, and
  • previously treated (N=41), had an ORR of 85.4% with a median DOR of 26.7 months.5

Efficacy Results Per Independent Review Committee Assessment in Patients With RET Fusion-Positive Thyroid Cancer in LIBRETTO-001 presents efficacy results for RET fusion-positive thyroid cancer.

Efficacy Results Per Independent Review Committee Assessment in Patients With RET Fusion-Positive Thyroid Cancer in LIBRETTO-0015

Outcome Measureab

Treatment-Naïvec

(N=24)

Pre-treated

(N=41)

ORR, % (95% CI)

95.8 (78.9, 99.9)

85.4 (70.8,94.4)

Best overall response, n (%)

Complete response

5 (20.8)

5 (12.2)

Partial response

18 (75.0)

30 (73.2)

Stable disease

1 (4.2)

6 (14.6)

Progressive disease

0 (0.0)

0 (0.0)

Not evaluable

0 (0.0)

0 (0.0)

PFS

Median PFS, months (95% CI)

NE (44.2,NE)

27.4 (14.5,NE)

Median duration of follow-up, months

24.9

30.4

DOR 

Median DOR, months (95% CI)

NE (42.8,NE)

26.7 (12.1,NE)

Median duration of follow-up, months

17.8

33.9

Abbreviations: DOR = duration of response; NE = not estimable; ORR = objective response rate; PFS = progression-free survival; RET = rearranged during transfection.

aData cutoff date of January 2023.

bEfficacy population includes all patients enrolled 6 months prior to data cutoff date.

cPatients naïve to any systemic therapy other than radioactive iodine.

Efficacy of Selpercatinib in RET-Mutant Medullary Thyroid Cancer

In the January 2023 data cutoff of the phase 1/2 LIBRETTO-001 trial, patients with RET-mutant MTC

  • who were treatment-naïve (N=116), had an ORR of 84.5% with a median DOR that was not estimable
  • who were cabozantinib/vandetanib-naïve (N=143), had an ORR of 82.5% with a median DOR that was not estimable, and
  • previously treated with cabozantinib/vandetanib (N=152), had an ORR of 77.6% with a median DOR of 45.3 months.5

Efficacy Results Per Independent Review Committee Assessment in Patients With RET-Mutant Medullary Thyroid Cancer in LIBRETTO-001 presents efficacy results for RET-mutant MTC.

Efficacy Results Per Independent Review Committee Assessment in Patients With RET-Mutant Medullary Thyroid Cancer in LIBRETTO-0015

Outcome Measureab

Treatment-Naïvec

(N=116)

CAB/VAN-Naïved

(N=143)

Prior CAB and/or VANe

(N=151)

ORR, % (95% CI)

84.5 (76.6,90.5)

82.5 (75.3,88.4)

77.6 (70.2,84.0)

Best overall response, n (%)

Complete response

30 (25.9)

34 (23.8)

19 (12.5)

Partial response

68 (58.6)

84 (58.7)

99 (65.1)

Stable disease

13 (11.2)

20 (14.0)

25 (16.4)

Progressive disease

2 (1.7)

2 (1.4)

2 (1.3)

Not evaluable

3 (2.6)

3 (2.1)

7 (4.6)

PFS

Median PFS, months (95% CI)

NE (51.3,NE)

NE (51.3,NE)

41.4 (30.2,NE)

Median duration of follow-up, months

41.6 

42.4

44.0

DOR

Median DOR, months (95% CI)

NE (51.3,NE)

NE (51.3,NE)

45.3 (33.6,NE)

Median duration of follow-up, months

38.0

39.4

38.3

Abbreviations: CAB = cabozantinib; DOR = duration of response; NE = not estimable; ORR = objective response rate; PFS = progression-free survival; RET = rearranged during transfection; VAN = vandetanib.

aData cutoff date of January 2023.

bEfficacy population includes all patients enrolled 6 months prior to data cutoff date.

cPatients naïve to any systemic therapy.

dPatients not previously treated with cabozantinib and/or vandetanib.

ePatients previously treated with cabozantinib and/or vandetanib.

Calcitonin and Carcinoembryonic Antigen Response in LIBRETTO-001

LIBRETTO-001 evaluated biochemical response rates for calcitonin and carcinoembryonic antigen (CEA) (Biochemical Response in Patients With RET-Mutant Medullary Thyroid Cancer in LIBRETTO-001).

Biochemical Response in Patients With RET-Mutant Medullary Thyroid Cancer in LIBRETTO-0016,7

Response, n (%)ab

CAB/VAN-Naïve

Prior CAB and/or VAN
Overall
(N=151)

Overall
(N=142)

Treatment-Naïve
(N=115)

Calcitonin
(N=142)

CEA
(N=136)

Calcitonin
(N=115)

CEA
(N=111)

Calcitonin
(N=148)

CEA
(N=146)

Biochemical response rate, % (95% CI)c

95.1
(90.1,98.0)

79.4
(71.6,85.9)

94.8
(89.0,98.1)

78.4
(69.6,85.6)

90.1
(86.3,95.7)

74.0
(66.1,80.9)

Best biochemical response, n (%)d

CR

49 (34.5)

29 (21.3)

43 (37.4)

26 (23.4)

41 (27.7)

22 (15.1)

PR

86 (60.6)

79 (58.1)

66 (57.4)

61 (55.0)

95 (64.2)

86 (58.9)

SD

1 (0.7)

18 (13.2)

0

15 (13.5)

1 (0.7)

23 (15.8)

Median time to response, months (range)e

0.5
(0.4,9.3)

1.9
(0.4,16.7)

0.5
(0.4,9.3)

1.9
(0.4,14.7)

0.5
(0.4,6.2)

1.0
(0.4,41.4)

Abbreviations: CAB = cabozantinib; CEA = carcinoembryonic antigen; CR = complete response; MTC = medullary thyroid cancer; PR = partial response; RET = rearranged during transfection; SD = stable disease; VAN = vandetanib. 

aData cutoff date of June 2021.

bEvaluable patients include RET-mutant MTC patients with abnormal baseline value of calcitonin. Patients with normal calcitonin values were excluded from this analysis.

cBiochemical response rate refers to a change from baseline in serum tumor markers maintained for ≥4 weeks; different types of responses are CR = normalization; PR = ≥50% reduction; SD = between -50% to +50% change.

dComplete response + partial response.

eDefined as the number of months elapsed between the date of the first dose of selpercatinib and the first documentation of biochemical response (CR or PR, whichever occurs first) that was confirmed a minimum of 4 weeks later.

Case Report of Selpercatinib Response in Brain Metastasis in Patient With Medullary Thyroid Cancer

A 67-year-old female patient with high calcitonin and CEA was diagnosed with RET M918T-mutant and CDKN2C gene deletion MTC that had metastasized to the lymphatic system. A thyroidectomy was performed, but her calcitonin levels continued to increase. Imaging showed lesions in

  • the right lower lung
  • liver
  • spine, and
  • right caudate nucleus in the brain.

She received whole brain radiation, external beam radiation to her spine, and was started on cabozantinib.8

She experienced numerous side effects which led to cabozantinib dose reductions, but she achieved partial response per RECIST 1.1 criteria. After 8 months, she experienced disease progression. She was enrolled into the LIBRETTO-001 clinical trial, and selpercatinib 160 mg twice daily was initiated.8

The patient experienced clinical response within one month with resolution of the diarrhea and nausea, and increased appetite. Her CEA levels also decreased. Imaging showed near complete resolution of the previously diagnosed brain metastases at 8 weeksm, and complete resolution of the brain metastases and leptomeningeal lesion at T11 of her spine was observed at 33 weeks. Partial extracranial response assessed by RECIST 1.1 was seen at 1 year after selpercatinib therapy.8

Imaging at 17 months revealed a new brain lesion that was treated by stereotactic radiosurgery (SRS) and continued selpercatinib. At 20 months, imaging revealed new spine and liver lesions, and her calcitonin levels were elevated. Testing showed RET M918T missense mutation. She continued to experience central nervous system response until 22 months after starting selpercatinib when new brain lesions were found. She received SRS, and selpercatinib was continued because of the clinical benefit she felt it provided. The patient tolerated treatment well and reported grade 1 fatigue and leukopenia which was attributed to selpercatinib.8

Safety of Selpercatinib in RET-Altered Thyroid Cancer 

Two patients (3%) with RET fusion-positive thyroid cancer discontinued treatment due to TEAE and 30 patients (9.3%) with RET-mutant MTC discontinued treatment due to TEAEs.5 Treatment-emergent Adverse Events of Any Grade in ≥25% of Patients in LIBRETTO-001 summarizes the most common TEAEs occurring in ≥25% of the LIBRETTO-001 safety population. 

Treatment-emergent Adverse Events of Any Grade in ≥25% of Patients in LIBRETTO-0015

RET Fusion-Positive Thyroid Cancer

(N=66)

RET-Mutant Medullary Thyroid Cancer

(N=324)

TEAE, n (%)a

Any grade

Grade ≥3 

Any grade

Grade ≥3 

Diarrhea

36 (54.5)

5 (7.6)

154 (47.5)

22 (6.8)

Dry mouth

33 (50.0)

0

140 (43.2)

0

Hypertension

31 (47.0)

10 (15.2)

150 (46.3)

70 (21.6)

Fatigue

29 (43.9)

1 (1.5)

149 (46.0)

12 (3.7)

Constipation

27 (40.9)

0

139 (42.9)

1 (0.3)

Abdominal Pain

24 (36.4)

3 (4.5)

109 (33.6)

10 (3.1)

Vomiting

24 (36.4)

2 (3.0)

94 (29.0)

8 (2.5)

Nausea

20 (30.3)

0

127 (39.2)

5 (1.5)

Arthralgia

19 (28.8)

1 (1.5)

102 (31.5)

2 (0.6)

Abbreviations: RET = rearranged during transfection; TEAE = treatment-emergent adverse event.

aData cutoff date of January 2023.

Baseline Characteristics of Patients With RET-Altered Thyroid Cancer

Baseline Characteristics for Patients with RET Fusion-Positive Thyroid Cancer in LIBRETTO-001 presents baseline characteristics for the RET fusion-positive thyroid cancer cohort.

Baseline Characteristics for Patients with RET Fusion-Positive Thyroid Cancer in LIBRETTO-0015,7

Characteristica

Treatment-Naïveb

(N=24)

Pre-treated

(N=41)

Median age, years (range)

60.5 (20-84)

58.0 (25-88)

Sex, n (%)

Male

14 (58.3)

18 (43.9)

Female

10 (41.7)

23 (56.1)

Race, n (%)

White

18 (75.0)

24 (58.5)

Asian

1 (4.2)

12 (29.3)

Black or African American

0 (0.0)

3 (7.3)

Primary Diagnosis, n (%)

Papillary Thyroid Cancer

23 (95.8)

31 (75.6)

Anaplastic Thyroid Cancer

0

4 (9.8)

Poorly Differentiated Thyroid Cancer

1 (4.2)

5 (12.2)

Hurthle Cell Thyroid Cancer

0

1 ( 2.4)

Prior Systemic Regimens, median (range)

1 (0-5)

3 (1-7)

Prior Systemic Therapy, n (%)

Multitargeted Kinase Inhibitor

0 (0.0)

35 (85.4)

Radioiodine

18 (75.0)

30 (73.2)

Anti-PD1/PD-L1 Therapy

0 (0.0)

3 (7.3)

Metastatic Disease, n (%)

24 (100)

36 (87.8)

RET fusion partner, n (%)

CCDC6

15 (62.5)

25 (61.0)

NCOA4

7 (29.2)

8 (19.5)

Other/Unknown

2 (8.3)

8 (19.5)

Abbreviations: PD-1/PD-L1 = programmed death-1/programmed death-ligand 1; RET = rearranged during transfection.

aData cutoff date of January 2023.

bPatients naïve to any systemic therapy other than radioactive iodine.

Baseline Characteristics for Patients with RET-Mutant Medullary Thyroid Cancer in LIBRETTO-001 presents baseline characteristics for the RET-mutant MTC cohort.

Baseline Characteristics for Patients with RET-Mutant Medullary Thyroid Cancer in LIBRETTO-0015

Characteristic 

Treatment-Naïvea

(N=116)

CAB/VAN-Naïvebb

(N=143)

Prior CAB and/or VANc
(N=151)

Median age, years (range)

57.0 (15-87)

57.0 (15-87)

58.0 (17-90)

Sex, n (%)

Male

71 (61.2)

83 (58.0)

97 (63.8)

Female

45 (38.8)

60 (42.0)

55 (36.2)

Race, n (%)

White

100 (86.2)

124 (86.7)

137 (86.7)

Asian

6 (5.2)

8 (5.6)

2 (1.3)

Black or African American

2 (1.7)

2 (1.4)

2 (1.3)

Prior Systemic Regimens, median (range)

0 (0-0)

0 (0-2)

2 (1-8)

Prior Systemic Therapy, n (%)

Multitargeted Kinase Inhibitor

0 (0)

9 (6.3)

152 (100)

Metastatic Disease, %

109 (94.0)

134 (93.7)

141 (92.8)

RET mutation type, n (%)

M918T

66 (56.9)

86 (60.1)

99 (65.1)

Extracellular cysteine mutation

29 (25.0)

34 (23.8)

24 (15.8)

V804 M/L

5 (4.3)

6 (4.2)

8 (5.3)

Other

16 (13.8)

17 (11.9)

21 (13.8)

Abbreviations: CAB = cabozantinib; RET = rearranged during transfection; VAN = vandetanib.

aPatients naïve to any systemic therapy.

bPatients not previously treated with cabozantinib and/or vandetanib.

cPatients previously treated with cabozantinib and/or vandetanib.

LIBRETTO-001 Phase 1/2 Selpercatinib Use in RET-Altered Thyroid Cancer

LIBRETTO-001 is a multicenter, open-label, phase 1/2 study of selpercatinib administered orally to patients with RET fusion-positive solid tumors, RET-mutant MTC, and other tumors with RET activation.9-12

LIBRETTO-001 Study Design  presents the LIBRETTO-001 study design.

LIBRETTO-001 Study Design13 

Figure description: 

The study design for LIBRETTO-001 is presented. The safety population includes all patients enrolled with RET-altered cancers. Two cohorts included patients with RET-mutant MTC and RET fusion-positive thyroid cancers. Both groups included previously treated and treatment-naïve patients. The primary endpoint is objective response rate.

Abbreviations: BID = twice daily; cabo = cabozantinib; ECOG PS = Eastern Cooperative Oncology Group performance status; FISH = fluorescence in situ hybridization; IAS = integrated analysis set; MTC = medullary thyroid cancer; NGS = next generation sequencing; ORR = objective response rate; PAS = primary analysis set; PCR = polymerase chain reaction; QD = daily; QTc =  QT interval corrected for heart rate (Fridericia method); RAI = radioactive iodine; RECIST = Response Evaluation Criteria in Solid Tumors; RET = rearranged during transfection; TC= thyroid cancer; vande = vandetanib.

a Safety population includes all patients who received at least one selpercatinib dose prior to Jan 2023 data cutoff . bEfficacy population includes all patients enrolled 6 months prior to data cutoff date, to allow adequate follow-up.

*The PAS is a subset of the IAS and was defined through health authority agreement as the first 55 consecutively enrolled patients with RET-mutant MTC previously treated with cabo/vande and is the more mature dataset. Patients with nonmeasurable disease enrolled in phase 1 were included in the PAS.




Treatment beyond progression was permitted with continued benefit.9,10

Enclosed Prescribing Information

RETEVMO® (selpercatinib) capsules, for oral use, Lilly

References

The published references below are available by contacting 1-800-LillyRx (1-800-545-5979).

1Hadoux J, Elisei R, Brose M, et al; LIBRETTO-531 Trial Investigators. Phase 3 trial of selpercatinib in advanced RET-mutant medullary thyroid cancer. N Engl J Med. Published online October 21, 2023. www.nejm.org/doi/full/10.1056/NEJMoa2309719

2Hadoux J, Elisei R, Hoff A, et al. Efficacy of selpercatinib by RET mutation in RET-Mutant Medullary Thyroid Cancer: A combined analysis of LIBRETTO-001 AND LIBRETTO-531 trials. Poster presented at: 2024 American Thyroid Association (ATA); October 30-November 4; Chicago, IL.

3Wirth LJ, Brose MS, Elisei R, et al. LIBRETTO-531: a phase III study of selpercatinib in multikinase inhibitor-naïve RET-mutant medullary thyroid cancer. Future Oncol. 2022;18(28):3143-3150. https://doi.org/10.2217/fon-2022-0657 

4A study of selpercatinib (LY3527723) in participants with RET-mutant medullary thyroid cancer (LIBRETTO-531). ClinicalTrials.gov identifier: NCT04211337. Updated October 30, 2023. Accessed November 3, 2023. https://clinicaltrials.gov/ct2/show/NCT04211337

5Wirth LJ, Subbiah V, Worden F, et al. Efficacy of selpercatinib in patients with medullary thyroid cancer (MTC): update of the LIBRETTO-001 trial. Presented at: the European Society for Medical Oncology (ESMO); Madrid, Spain; October 20-24, 2023.

6Kroiss M, Sherman E, Wirth LJ, et al. Durable efficacy of selpercatinib in patients (pts) with medullary thyroid cancer (MTC): update of the LIBRETTO-001 trial. Presented at: the European Society for Medical Oncology (ESMO); Paris, France; September 9-13, 2022.

7Data on file, Eli Lilly and Company and/or one of its subsidiaries.

8Andreev-Drakhlin A, Cabanillas M, Amini B, Subbiah V. Systemic and CNS activity of selective RET inhibition with selpercatinib (LOXO-292) in a patient with RET-mutant medullary thyroid cancer with extensive CNS metastases. JCO Precis Oncol. 2020;4:1302-1306. https://dx.doi.org/10.1200/PO.20.00096

9Wirth LJ, Sherman E, Robinson B, et al. Efficacy of selpercatinib in RET-altered thyroid cancers. N Engl J Med. 2020;383(9):825-835. https://dx.doi.org/10.1056/NEJMoa2005651

10Drilon 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. https://dx.doi.org/10.1056/NEJMoa2005653

11A study of selpercatinib (LOXO-292) in participants with advanced solid tumors, RET fusion-positive solid tumors, and medullary thyroid cancer (LIBRETTO-001). ClinicalTrials.gov identifier: NCT03157128. Updated March 4, 2024. Accessed March 5, 2024. https://www.clinicaltrials.gov/ct2/show/NCT03157128

12Retevmo [package insert]. Indianapolis, IN: Eli Lilly and Company; 2024.

13Sherman E, Wirth L, Shah M, et al. Selpercatinib efficacy and safety in patients with RET-altered thyroid cancer: a LIBRETTO-001 update. Poster presented at: 57th Annual Meeting of the American Society of Clinical Oncology (ASCO Virtual); June 4-8, 2021. Accessed November 9, 2022. https://assets.ctfassets.net/mpejy6umgthp/3Akm5uCVsGOJEwrbsmT1Zh/2b3be4e81531356578012b689702141a/SELPT1_ASCO2021_Sherman.pdf

Date of Last Review: October 24, 2024

Additional related information:

  • Selpercatinib (LOXO-292) in Patients with RET-altered Thyroid Cancers
  • Intracranial Activity of Selpercatinib (LOXO-292) in RET Fusion-Positive Non-small Cell Lung Cancer (NSCLC) Patients on the LIBRETTO-001 Trial
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