Q3 2020 Sales Performance
Tumor volume (mm³)
Zejula
A unique PK profile may explain the benefit in HR-proficient patients
1200-
1000-
BRCAmut TNBC model
MDA-MB-436 (BRCA1mut)
• Vehicle (n=6)
• Niraparib (75 mg/kg qd n=6)
Olaparib (75/67 mg/kg bid n=6)
800-
600-
400-
200-
0
0
5
10
15
20
25
30
Time (days)
Tumor volume (mm³)
gsk
BRCAwt ovarian model
A2780 (BRCAwt)
3000-
Vehicle (n=15)
2500-
Niraparib (62.5 mg/kg qd n=6)
Olaparib (100 mg/kg qd n=6)
2000-
P=0.005**
1500-
1000-
500-
0
°
2
10
Time (days)
www.oncotarget.com
Oncotarget, 2018, Vol. 9, (No. 98), pp: 37080-37096
Research Paper
A comparative pharmacokinetic study of PARP inhibitors
demonstrates favorable properties for niraparib efficacy in
preclinical tumor models
Kaiming Sun, Keith Mikule', Zebin Wang, Grace Poon', Aparajitha Vaidyanathan²,
Gillian Smith', Zhi-Yi Zhang', Jeffrey Hanke, Sridhar Ramaswamy' and Jing Wang
"Our results show that at steady state, tumor
exposure to niraparib is 3.3 times greater than
plasma exposure in tumor xenograft mouse models.
In comparison, the tumor exposure to olaparib is less
than observed in plasma. In addition, niraparib
crosses the blood-brain barrier and shows good
sustainability in the brain, whereas sustained brain
exposure to olaparib is not observed in the same
models.
Consistent with its favourable tumor and brain
distribution, niraparib achieves more potent tumor
growth inhibition than olaparib in BRCAwt models
and an intracranial tumor model at maximum
tolerated doses."
Sun et al
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