1. Bibliography of Publications by Ravi S. Harapanhalli, Ph.D.
Original Peer Reviewed Articles:
1. Harapanhalli RS. Synthesis of erivanin and 1-epierivanin from 1-(α)-santonin. J Chem
Soc Perkin Trans 1988;1:2633-7.
2. Harapanhalli RS. Approach to the synthesis of side-chain eudesmanediols: synthesis of
kudtriol from 1-(α)-santonin. J Chem Soc Perkin Trans 1988;1:3149-53.
3. Harapanhalli RS. Synthetic transformation of santonin into (5 α, 7 α, 11β )-3,6-
dioxogermacr-1-en-13, 7-olide, a new intermediate for germacranes and guaianes.
Liebigs Ann Chem 1988; 1009-11.
4. Harapanhalli RS. Synthesis of some new eudesmanoate intermediates of cis-series from
(–)-(α)-santonin. Ind J Chem 1988;27B:884-6.
5. Narra VR, Howell RW, Harapanhalli RS, Sastry KSR, Rao DV. Radiotoxicity of some
iodine-123, iodine-125 and iodine-131-labeled compounds in mouse testes: implications
for radiopharmaceutical design. J Nucl Med 1992;33:2196-201.
6. Harapanhalli RS, Narra VR, Howell RW, Rao DV. [35
S]cysteamine: facile synthesis, in
vivo biokinetics, and subcellular distribution. Nucl Med Biol 1993;20:117-24.
7. Harapanhalli RS, Yaghmai V, Patel YD, Baker SR, Rao DV. Assay of radiographic
contrast agents in mice plasma and testes by high-performance liquid chromatography.
Anal Chem 1993;65:606-12.
8. Harapanhalli RS, Howell RW, Rao DV. Testicular and plasma ascorbic acid levels in
mice following dietary intake: a high-performance liquid chromatographic analysis. J
Chromatogr 1993;614:233-43.
9. Yaghmai V, Harapanhalli RS, Patel YD, Baker SR, Rao DV. Effects of diatrizoate and
iopamidol on spermatogenesis. Invest Radiol 1993;28:1160-4.
10. Narra VR, Harapanhalli RS, Howell RW, Sastry KSR, Rao DV. Vitamins as
radioprotectors in vivo. I. Protection by vitamin C against internal radionuclides in mouse
testes: implications to the mechanism of damage caused by the Auger effect. Radiat Res
1994;137:394-9.
11. Harapanhalli RS, Howell RW, Rao DV. bis-Benzimidazole dyes, Hoechst 33258 and
Hoechst 33342: radioiodination, facile purification and subcellular distribution. Nucl
Med Biol 1994;21:641-7.

2. 12. Harapanhalli RS, Narra VR, Yaghmai V, Azure MT, Goddu SM, Howell RW, Rao DV.
Vitamins as radioprotectors in vivo II. Protection by vitamin A and soybean oil against
radiation damage caused by internal radionuclides. Radiat Res 1994;139:115-22.
13. Narra VR, Harapanhalli RS, Goddu SM, Howell RW, Rao DV. Radioprotection against
biological effects of internal radionuclides in vivo by S-(2-aminoethyl)isothiouronium
bromide hydrobromide (AET). J Nucl Med 1995;36:259-66.
14. Harapanhalli RS, Schafranek W, Ong GL, Mattes MJ. Lysine-directed radioiodination
of proteins with a cyanuric chloride derivative of aminofluorescein. Anal Biochem 1995;
231:50-6.
15. Harapanhalli RS, McLaughlin LW, Howell RS, Rao DV, Adelstein SJ, Kassis AI.
[125
I/127
I]iodoHoechst 33342: synthesis, DNA binding, and biodistribution. J Med Chem
1996;39:4804-9.
16. Harapanhalli RS, Yaghmai V, Giuliani D, Howell RW, Rao DV. Antioxidant effects of
vitamin C in mice following X-irradiation. Res Commun Mol Pathol Pharmacol
1996;94:271-87.
17. Goddu MS, Narra VR, Harapanhalli RS, Howell RW and Rao DV. Radioprotection by
DMSO against the biological effects of incorporated radionuclides in vivo-comparison
with other radioprotectors and evidence for indirect action of Auger electrons. Acta
Oncologica 1996;35;901-908.
18. Kandarpa K, Nakatsuka S, Bravo SM, Harapanhalli RS, and Barry JJ. Mural delivery of
iloprost with use of hydrogel-coated balloon catheters suppresses local platelet
aggregation. J Vasc Interv Radiol. 1997; 8(6): 997-1004.
19. Harapanhalli RS, Adelstein SJ and Kassis AI. Site-specific conjugation of ethidium
homodimer to B72.3 Mab: Retention of immunoreactivity, isoelectric point and tumor
targeting. Radiochimica Acta, 1997; 79:73-76.
20. Harapanhalli RS, Matalka KZ, Jones PL, Mahmood A, Adelstein SJ, and Kassis AI.
Modification of in-vivo behavior of an antibody immunoconjugate following alteration of
its isoelectric point. Radiochimica Acta, 1997; 79: 77-82.
21. Harapanhalli RS, Matalka KZ, Jones PL, Mahmood A, Adelstein SJ, and Kassis AI.
Modification of in-vivo behavior of an antibody immunoconjugate following alteration of
its isoelectric point. Nucl Med Biol, 1998; 25: 267-278.
22. Harapanhalli RS, Roy AR, Adelstein SJ and Kassis AI. 131
I/127
I-iodorhodamine 123:
Synthesis, Cellular localization and biodistribution in tumor-bearing athymic mice.
Comparative biodistribution with 99m
Tc-MIBI. J Med Chem, 1998; 41, 2111-2117.
23. Kassis AI, Harapanhalli RS and Adelstein SJ. Comparison of strand breaks in plasmid
DNA following positional changes of Auger electron-emitting Iodine-125. Radiat Res,
1999, 151, 167-176.

3. 24. Kassis AI, Harapanhalli RS and Adelstein SJ. Strand breaks in plasmid DNA following
positional changes of Auger-electron-emitting iodine-125: Direct versus Indirect effects.
Radiat Res, 1999, 152, 530-538.
25. Walicka MA, Ding Y, Roy AM, Harapanhalli, RS, Adelstein SJ, and Kassis AI.
Cytotoxicity of 125
I-iodoHoechst 33342: Contribution of scavengeable effects. Int. J.
Radiat. Biol., 1999, 75, 1579-1587.
26. Nan Hui, Harapanhalli RS, Dahman BA, Kai Chen, Ketai Wang, Adelstein SJ, and
Kassis AI. Synthesis and Biological Evaluation of a Radioiodinated Quinazolinone
Derivative for Enzyme-mediated Insolubilization Therapy. Bioconjugate Chem., 2002, 13,
357-364.
27. Kaminskas, E., Lechleider, R., Jiang, X., Aziz, R., Bullock, J., Kasliwal, R.,
Harapanhalli, R., Pope, S., Sridhara, R., Booth, B., Leighton, J., Dagher, R., Justice, R.,
and Pazdur, R. Approval Summary: Ixabepilone for Treatment of Advanced Breast
Cancer Refractory to Previous Chemotherapies. Clinical Cancer Research (accepted for
publication)
28. Brave, M., Goodman, V., Kaminskas, E., Farrell, A., Timmer, W., Pope, S.,
Harapanhalli, R., Saer, H., Morse, D., Bullock, J., Men, A., Noory, C., Ramachandani,
R., Kenna, L., Booth, B., Gobburu, J., Jiang, X., Sridhara, R., Justice, R., and Pazdur, R.
Sprycel for Chronic Myeloid Leukemia and Philadelphia Chromosome-Positive Acute
Lymphoblastic Leukemia Resistant to or Intolerant of Imatinib Mesylate. Clinical Cancer
Research 2008, 14, 352-359.
29. Mann, B.S., Johnson, J.R., He, K., Sridhara, R., Abraha, S., Booth, B.P., Verbois, L.,
Morse, D.E., Jee, J.M., Pope S., Harapanhalli, R.S., Dagher, R., Farrell, A., Justice, R,
and Pazdur, R. Vorinostat for Treatment of Cutaneous Manifestations of Advanced
Primary Cutaneous T-cel Lymphoma. Clinical Caner Research, 2007, 13, 18-22.
30. Ravi S. Harapanhalli, Making Sense of FDA’s Post-market Surveillance Program.
Regulatory Focus, Regulatory Affairs Professionals Society, 1-6, September 2009
31. Ravi S. Harapanhalli, Food and Drug Administration Requirements for Testing and
Approval of New Radiopharmaceuticals. Seminars in Nuclear Medicine, 40: 364-384,
2010
Manuscripts pending publication:
32. Kassis AI, Harapanhalli RS, Matalka KZ, Mahmood A, Jones PL and Adelstein SJ. A
novel antibody-dependent approach for radiotargeting tumor xenografts via intercalator-
DNA bridging. J Nucl Med.
33. Harapanhalli RS, Matalka KZ, Adelstein SJ, and Kassis AI. Conjugation of ethidium
homodimer to B72.3 MAb via Fc-directed peptide hapten: DNA binding,
immunoreactivity, isoelectric point and in vivo tumor targeting. Bioconj Chem.

4. 34. Harapanhalli RS, Roy A, Adelstein SJ, and Kassis AI. Long-chain analogs of
iodohoechst 33342: Synthesis, Radioiodination, DNA binding and cellular localization.
Bioorg. Med Chem Letts.
35. Harapanhalli RS, Adelstein SJ, and Kassis AI. Re-investigation of synthesis of 125
I-
Iododeoxyuridine by direct electrophillic iodination, and its targeting of liver-metastatized
CX-1 tumors in mice. Nucl Med Biol.
36. Harapanhalli RS, Terzian C, Adelstein SJ, and Kassis AI. Apoptosis induced in human
lymphocytes exposed to 99m
Tc-MIBI. Rad Res.
37. Harapanhalli RS, Yaghmai V, Guiliani D, Howell RW and Rao DV. Cysteamine does
not protect marrow cells from 32
P In Vivo. Radiat Res.
Proceedings of Meetings:
1. Howell RW, Narra VR, Hou D-Y, Terrone DA, Harapanhalli RS, Sastry KSR, Rao DV.
Relative biological effectiveness of Auger emitters for cell inactivation: in vitro versus in
vivo. In: Howell RW, Narra VR, Sastry KSR, Rao DV, eds. Biophysical aspects of
Auger processes. Woodbury, NY: American Institute of Physics, Incorporated, 1992:290-
318.
2. Narra VR, Harapanhalli RS, Howell RW, Sastry KSR, Rao DV. Chemical protection
against radionuclides in vivo: implications to the mechanism of Auger effect. In: Howell
RW, Narra VR, Sastry KSR, Rao DV, eds. Biophysical aspects of Auger processes.
Woodbury, NY: American Institute of Physics, Incorporated, 1992:319-35.
US. Patent:
U. S. Patent Application No.: 09/839,779
Title: Methods for Tumor Diagnosis and Therapy
Date filed: April 20, 2001
Investors: Amin Kasis and Ravi Harapanhalli
Book Chapters:
Harapanhalli, Ravi S. “Regulatory Considerations in the Development of Low-dose Solid Oral
Drug Products” in “Formulation and Analytical Development for Low Dose Oral Drug Products”
Edited by Jack Zheng, John Wiley and Sons, 2009.