Table 1.Status of Marine-Derived Natural Products in Clinical and Preclinical Trials Compound Name Source Status(Disease) Comment Bryostatin 1 Phase ll(Cancer) licensed to Bugula neritina TZT-1027 Synthetic Dolastatin Phase ll(Cancer) Also known as Auristatin PE and Soblidotin Cematodin Synthetic derivative Phase I/Il(Cancer) Some positive effects in melanoma of Dolastatin 15 ILX651,Synthatodin g hase I/ll (Cancer) Ecteinascidin 743 Ascidian Phase ll/ll(Cancer】 Licensed to Ortho Biotech(1&l/lanssen Ecteinascidia turhinata in2003.2005 Pharmaceuticals) Aplidine Phase ll(Cancer) Dehydrodidemnin B:made by total synthesis E7389 Sponge Phase ll (Cancer) Eisai's synthetic halichondrin B derivative Lissodendoryx sp. breast and lung Discodermolide Phase I(Cancer) Licensed to Novartis by Harbor Branch ermia dissoluta Kahalalide F Mollusk Evlsia rufescens Phase ll(Cancer) Licensed to PharmaMar by University of Hawaii and Alga Bryopsis sp. Zalypsis PhaseI(Cancer) PharmaMar(based on saframycin molecule) E5-285 Spisula polynyma Phase I(Cancer) Rho-GTP inhibitor KRN-7000 Phase I(Cancer) An agelasphin derivative Squalamine Sharl hase ll (Cancer) Anti-angiogenic activity as wel Squalus acanthias -941(Neovastat) Shark Phase ll/Ill(Cancer Defined mixture of<500 kDa from cartilage anti-angiogenic NVP-LAQ824 Synthetic PhaseI(Cancer) Derived from Psammaplin,Trichostatin and Irapoxin structures E-7974(isa0 Synthetic Phase l(Cancer) Carboxylate-end modified hemisasterlin hasel(Cancer Prot asome inhibitor Nereus Pharma GTS-21(aka DMBX) Marine worm PhaseI(Alzheimer's) Licensed to Taiho by the University of Florida 1) hase ll(anti-asthmatic Derivative of contignasterol,Inflazyme Pharma Petrosia contignata 1PL-512.602 Derivative of 576092 Phase ll(anti-asthmatic) With Aventis.no further data as of 08/2005 IPL-550,260 Derivative of 576092 Phase I(anti-asthmatic) With Aventis.No further data as08/2005 Ziconotide Mollusk Approved EDA 28DEC04 Licensed by Elan to Warner Lambert:launched (aka Prialt) Conus magus (Neuropathic pain) in U.S.and Europe in 2005 CGX-1160 Conus geographus Phase I(Pain) Corporation(lreland) ACV1 Conus victorae Phase I (Pain) Metabolic Pharma(Australia)(06/2006). conotoxin Vc1.1 This table was adapted from information kindly provided by David I.Ne National Cancer Institute.Bethesda.MD.USA 116 Occanography I Vol 19,No.2.June 2006116 Oceanography Vol. 19, No. 2, June 2006 Table 1. Status of Marine-Derived Natural Products in Clinical and Preclinical Trials Compound Name Source Status (Disease) Comment Bryostatin 1 Bryozoan Bugula neritina Phase II (Cancer) Now in combination therapy trials; licensed to GPC Biotech by Arizona State University TZT –1027 Synthetic Dolastatin Phase II (Cancer) Also known as Auristatin PE and Soblidotin Cematodin Synthetic derivative of Dolastatin 15 Phase I /II (Cancer) Some positive eff ects in melanoma ILX 651, Synthatodin Synthetic derivative of Dolastatin 15 Phase I/II (Cancer) For melanoma, breast, and non-small cell lung cancer (NSCLC) Ecteinascidin 743 Ascidian Ecteinascidia turbinata Phase II/III (Cancer) in 2003-2005 Licensed to Ortho Biotech (J&J/Janssen Pharmaceuticals) Aplidine Ascidian Aplidium albicans Phase II (Cancer) Dehydrodidemnin B; made by total synthesis E7389 Sponge Lissodendoryx sp. Phase II (Cancer) Eisai’s synthetic halichondrin B derivative; breast and lung Discodermolide Sponge Discodermia dissoluta Phase I (Cancer) Licensed to Novartis by Harbor Branch Oceanographic Institution Kahalalide F Mollusk Eylsia rufescens and Alga Bryopsis sp. Phase II (Cancer) Licensed to PharmaMar by University of Hawaii Zalypsis Synthetic Safracin B de￾rivative Phase I (Cancer) PharmaMar (based on saframycin molecule) ES-285 Spisula polynyma Phase I (Cancer) Rho-GTP inhibitor KRN-7000 Sponge Agelas mauritianus Phase I (Cancer) An agelasphin derivative Squalamine Shark Squalus acanthias Phase II (Cancer) Anti-angiogenic activity as well Æ-941 (Neovastat) Shark Phase II/III (Cancer) Defi ned mixture of < 500 kDa from cartilage; anti-angiogenic NVP-LAQ824 Synthetic Phase I (Cancer) Derived from Psammaplin, Trichostatin and Trapoxin structures E-7974 (Eisai) Synthetic Phase I (Cancer) Carboxylate-end modifi ed hemisasterlin Salinosporamide A (NPI-0052) Bacterium Salinispora tropica Phase I (Cancer) Proteasome inhibitor Nereus Pharma GTS-21 (aka DMBX) Marine worm Phase I (Alzheimer’s) Licensed to Taiho by the University of Florida IPL-576,092 (aka HMR-4011A) Sponge Petrosia contignata Phase II (anti-asthmatic) Derivative of contignasterol; Infl azyme Pharma IPL-512,602 Derivative of 576092 Phase II (anti-asthmatic) With Aventis. No further data as of 08/2005 IPL-550,260 Derivative of 576092 Phase I (anti-asthmatic) With Aventis. No further data as 08/2005 Ziconotide (aka Prialt) Mollusk Conus magus Approved FDA 28DEC04 (Neuropathic pain) Licensed by Elan to Warner Lambert; launched in U.S. and Europe in 2005 CGX-1160 Conus geographus Phase I (Pain) Cognetix and Elan Corporation (Ireland); Phase II late 2005 ACV1 Conus victoriae Phase I (Pain) Metabolic Pharma (Australia)(06/2006), conotoxin Vc1.1 Th is table was adapted from information kindly provided by David J. Newman, National Cancer Institute, Bethesda, MD, USA