Major R&D Pipeline: 3ADCs
ENHERTU®: NSCLC, CRC
DESTINY-Lung01 study (HER2 mutated/overexpressing, 2L+, Ph2): TLR obtained in June
Daiichi-Sankyo
HER2 mutated: Granted breakthrough therapy designation in US, filing strategy to be discussed with health authorities
HER2 overexpressing: Development strategy under discussion based on the data
Presented DESTINY-CRC01 study (HER2 expressing, 3L+, Ph2) final results at ASCO 2021
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DESTINY-CRC01 efficacy
DESTINY-CRC01 safety
Adverse Events in ≥20% of Patients
HER2 IHC3+ or IHC2+/ISH+
Cohort A (n = 53)
HER2 IHC2+/ISH-
Cohort B (n=15)
Any Grade
HER2 IHC1+
Cohort C (n = 18)
Best % Change From Baseline in the Sum
of Diameters of Measurable Tumors
-20
-40
-60
HER2 IHC3+ or IHC2+/ISH+ Cohort A (n = 49a)
-80
A
IHC3+
IHC2+/ISH+
Prior anti-HER2 treatment
-100
Overall
(N = 86)
n (%)
Any Grade
Any Grade
Patients with any TEAE
53 (100)
15 (100)
18 (100)
Any Grade
86 (100)
Grade ≥3
56 (65.1)
Nausea
37 (69.8)
9 (60.0)
7 (38.9)
53 (61.6)
5 (5.8)
Anemia
21 (39.6)
4 (26.7)
6 (33.3)
31 (36.0)
12 (14.0)
Fatigue
21 (39.6)
7 (46.7)
3 (16.7)
31 (36.0)
1 (1.2)
Decreased appetite
18 (34.0)
5 (33.3)
7 (38.9)
30 (34.9)
0
Platelet count decreased
17 (32.1)
4 (26.7)
7 (38.9)
28 (32.6)
8 (9.3)
Vomiting
23 (43.4)
3 (20.0)
1 (5.6)
27 (31.4)
1 (1.2)
Neutrophil count decreased
Diarrhea
20 (37.7)
2 (13.3)
4 (22.2)
26 (30.2)
19 (22.1)
19 (35.8)
0
4 (22.2)
23 (26.7)
1 (1.2)
Interstitial Lung Disease (ILD)
*
HER2 IHC2+/ISH+ with an NRAS mutation b
A
All Patients (N=86)
Grade 1
n (%)
0
a4 patients from the full analysis set were excluded since 1 patient had no measurable target lesion and 3 patients had no
postbaseline data. By local assessment.
Grade 2
4 (4.7)
Grade 3
1 (1.2)
Grade 4
0
Grade 5
Any Grade/Total
3 (3.5)a
8 (9.3)b.c
Promising efficacy profile, ORR 45.3%, mDOR 7 months,
mPFS 6.9 months, mOS 15.5 months, were observed in HER2
positive cohort (Cohort A)
Safety profile is consistent with the
known safety profile
Careful monitoring and prompt
intervention for ILD are required
AE, adverse events; ILD, interstitial lung disease a2 patients were from cohort A, 1 from cohort B. b4 patients were from
cohort A, 3 from cohort B and 1 from cohort C. CILD grades are the highest/most severe grade recorded in a patient.
CRC: colorectal cancer, DOR: duration of response, ORR: objective response rate, OS: overall survival, PFS: progression free survival, TLR: top line results
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