Hiroaki  Mitsuya, M.D., Ph.D.

Hiroaki Mitsuya, M.D., Ph.D.

  • Center for Cancer Research
  • National Cancer Institute
HIV and AIDS Malignancy Branch


In 1985, using an in vitro drug testing system involving human target cells that Dr. Hiroaki Mitsuya created, he showed for the first time that azidothymidine (AZT) had potent anti-HIV activity in vitro. Based on such data, AZT was ultimately selected for a clinical trial at the NCI and Dr. Mitsuya collaborated in a series of clinical studies, establishing AZT as the first drug for AIDS therapy. Concomitantly, Dr. Mitsuya discovered that 2',3'-dideoxynucleosides (ddNs) were active as a "family" against human immunodeficiency virus (HIV). Of these, ddI and ddC ultimately came into clinical use as important anti-HIV drugs.

Since these epochal studies, Dr. Mitsuya has continued to produce important insights into the therapy of HIV/AIDS.

Areas of Expertise

HIV/AIDS Therapeutics
Drug Resistance
Protease Inhibitors


Selected Recent Publications

The High Genetic Barrier of EFdA/MK-8591 Stems from Strong Interactions with the Active Site of Drug-Resistant HIV-1 Reverse Transcriptase

Takamatsu Y, Das D, Kohgo S, Hayashi H, Delino NS, Sarafianos SG, Mitsuya H, Maeda K.
Cell Chem Biol. 25(10): 1268-78, 2018. [ Journal Article ]

A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency

Aoki M, Hayashi H, Rao KV, Das D, Higashi-Kuwata N, Bulut H, Aoki-Ogata H, Takamatsu Y, Yedidi RS, Davis DA, Hattori SI, Nishida N, Hasegawa K, Takamune N, Nyalapatla PR, Osswald HL, Jono H, Saito H, Yarchoan R, Misumi S, Ghosh AK, Mitsuya H.
eLife. 6: e28020, 2017. [ Journal Article ]

Structural basis of HIV inhibition by translocation-defective RT inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA)

Salie ZL, Kirby KA, Michailidis E, Marchand B, Singh K, Rohan LC, Kodama EN, Mitsuya H, Parniak MA, Sarafianos SG.
Proc Natl Acad Sci U S A. 113(33): 9274-9, 2016. [ Journal Article ]

4'-modified nucleoside analogs: potent inhibitors active against entecavir-resistant hepatitis B virus

Takamatsu Y, Tanaka Y, Kohgo S, Murakami S, Singh K, Das D, Venzon DJ, Amano M, Higashi-Kuwata N, Aoki M, Delino NS, Hayashi S, Takahashi S, Sukenaga Y, Haraguchi K, Sarafianos SG, Maeda K, Mitsuya H.
Hepatology. 62(4): 1024-36, 2015. [ Journal Article ]

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