Table 1. Examples from literature of various antibody and antibody-drug conjugates’ permeability to the brain in preclinical models, with or without BBB disruption.

Antibody	Ab use	Drug	Model	Efficacy	Ref.
125I-MAb	Tracer	-	Normal rat brain	Permeability was increased with osmotic BBB disruption.	Neuwelt et al., 1986 [52]
125I-IgG 96.5125I-FAb 96.5125I-FAb 48.7				· Permeability increased with osmotic BBB disruption.· Enhanced & sustained retention of IgG in the brain.	Neuwelt et al., 1987 [53]
L6 IgGF(Ab’)2FAb			LX-1 human small-cell lung carcinoma intracerebral xenograft in nude rat	Antibody permeability to the brain increased with increased delay in dosing	Neuwelt et al.,1994 [54]
L6 IgG-conjugated iron oxine nanoparticles	Imaging (MRI)			Specific antibody displayed specific binding and potential for diagnostic enhancement of MRI	Remsen et al., 1996 [55]
SGN-15 MAb	Therapy	Doxorubicin		Immunoconjugate delivered across the BBB was effective against antigen-positive tumor cells	Neuwelt et al., 2003 [56]
Bevacizumab		Carboplatin	UW28 human glioma xenografts in nude rats	Combination therapy of Bevacizumab with carboplatin was more effective than Bevacizumab alone.	Jahnke et al., 2009 [57]
RituximabAnti-CD20	Therapy & Imaging (MRI)	Rituximabanti-CD20	Lymphoma rat model	Rituximab was effective at decreasing tumor volume and improving survival rate in a CNS lymphoma model	Muldoon et al., 2011 [58]
TDM1	Therapy	Emantsine	Her2+ BT474 or MDA-MB-361 CNS metastases in nude mice	TDM1 displayed increased survival rate in comparison to trastuzumab	Askoxylakis et al., 2015 [46]
89Zr-trastuzumabmuMAb 4D5TDM1	Tracer& Therapy	Emantsine	HER2-expressing transgenic Fo2-1282 or Fo5 mouse breast cancer in mice	· Trastuzumab displayed preferential uptake in tumor lessions· muMAb 4D5 and TDM1 significantly increased survival, as did combination therapy with PI3K/mTOR inhibitor GNE-317	Phillips et al., 2017 [59]