A.M.S. Mayer, Ph.D.
Professor of Pharmacology

Department of Pharmacology
Chicago College of Osteopathic Medicine
Midwestern University
555 31st Street
Downers Grove, IL 60515

 

Phone: (630) 515-6951
Fax: (630) 515-6295
E-mail: amayer@midwestern.edu

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MARINE PHARMACEUTICALS:
THE CLINICAL PIPELINE

As of June 2014, shown below are the marine-derived compounds which have been FDA-approved or are in Phase III, II or I of drug development and are part of the global marine pharmaceutical clinical pipeline since the review published by A.M.S. Mayer, K.B. Glaser, C. Cuevas, R.S. Jacobs, W. Kem, R.D. Little, J. M McIntosh, D.J. Newman, B.C. Potts and D. E. Shuster, Trends in Pharmacological Sciences, 31:255-265, 2010 ). Please note: Clinical trials with Soblidotin (TZT 1027), Tasidotin, Synthadotin (ILX-651), Hemiasterilin (E7974), Elisidepsin (Irvalec®), Pseudopterosin, and Plinabulin (NPI 2358) have been completed or discontinued (See http://clinicaltrials.gov/). Nereus Pharmaceuticals, Inc. (http://www.nereuspharm.com/ has been sold and no longer has a presence on the web.


Clinical
Status
Compound
Name
Trademark Marine
Organism
Chemical
Class
Molecular
Target
US - Active Clinical
Trials
Europe - Active Clinical
Trials
Disease
Area
Company/
Institution
FDA-Approved Brentuximab vedotin
(SGN-35)
Adcetris® Mollusk/
cyanobacterium
ADC(MMAE) CD30 & microtubules [43+] [15+] Cancer: Anaplastic large T-cell systemic maglinant lymphoma, Hodgkin's disease [Seattle Genetics]
Cytarabine
(Ara-C)
Cytosar-U® Sponge Nucleoside DNA polmerase [247+] [111+] Cancer:Leukemia [Bedford Laboratories]
Eribulin Mesylate (E7389) Halaven® Sponge Macrolide Microtubules [33+] [8+] Cancer: Metastatic Breast Cancer [Eisai Inc.]
Omega-3-acid ethyl esters Lovaza® Fish Omega-3 fatty acids Trygliceride-synthesizing enzymes [22+] [1+] Hypertriglyceridemia [GlaxoSmithKline]
Ziconotide Prialt® Cone snail Peptide N-Type Ca Channel [3+] [2+] Pain: Severe Chronic Pain Jazz Pharmaceuticals
Vidarabine
(Ara-A)
Vira-A® Sponge Nucleoside Viral DNA polymerase [103+] [2+] Antiviral: Herpes Simplex Virus No Link
Trabectedin
(ET-743)
(EU Registered only)
Yondelis® Tunicate Alkaloid Minor groove of DNA [12+] [22+] Cancer: Soft Tissue Sarcoma and Ovarian Cancer [Pharmamar]
Phase III
Plitidepsin Aplidin® Tunicate Depsipeptide Rac1 & JNK activation [2+] [4+] Cancer: Multiple Myeloma, Leukemia, Lymphoma [Pharmamar]
Tetrodotoxin Tectin® Pufferfish Guanidinium alkaloid Sodium Channel [2+] None Pain: Chronic Pain [Wex Pharmaceutical Inc.]
Phase II ABT-414 NA Mollusk/
cyanobacterium
ADC (MMAF) EGFR & microtubules [2+] None Cancer: Glioblastoma Multiforme, Squamous Cell Tumors No Link
PM00104 Zalypsis® Mollusk Alkaloid DNA-binding [1+] None Cancer: Uterine Cervical Cancer, Endometrial Cancer, Lymphoma [Pharmamar]
DMXBA
(GTS-21)
NA Worm Alkaloid α7 nicotinic acetylcholine receptor [1+] None Schizophrenia, Alzheimer Disease, Attention Deficit Hyperactivity Disorder, Endotoxemia, Sepsis, Vagal Activity No Link
Glembatumumab Vedotin
(CDX-011)
NA Mollusk/ cyanobacterium ADC (MMAE) GPNMB & microtubules [1+] None Cancer: Metastatic breast cancer, Metastatic melanoma, Triple negative breast cancer [Celldex Therapeutics]
PM01183 NA Tunicate Alkaloid Minor groove of DNA [7+] [4+] Cancer: Ovarian Cancer, Breast Cancer, Lung Cancer, Endometrial Cancer, Acute Leukemia [Pharmamar]
PSMA-ADC NA Mollusk/
cyanobacterium
ADC (MMAE) PSMA & microtubules [1+] None Cancer: Prostate cancer [Progenics Pharmaceuticals]
Phase I/II DNIB0600A NA Mollusk/ cyanobacterium ADC (MMAE) NaPi2b & microtubules [3+] [1+] Cancer: Non-Small Cell Lung Cancer, Ovarian Cancer; Epithelial Tumors, Malignant, Fallopian Tube Cancer, Peritoneal Neoplasms [Genentech/Roche]
Pinatuzumab vedotin
(DCDT-2980S)
NA Mollusk/ cyanobacterium ADC (MMAE) CD22 & microtubules None [1+] Cancer: Non-Hodgkin lymphoma, Chronic lymphocytic leukemia, Lymphoma, B-Cell, lymphoma, Follicular [Genentech/Roche]
Polatuzumab vedotin
(DCDS-4501A)
NA Mollusk/ cyanobacterium ADC (MMAE) CD79b & microtubules [1+] [1+] Cancer: Non-Hodgkin lymphoma, Chronic lymphocytic leukemia, Lymphoma, B-Cell, lymphoma, Follicular [Genentech/Roche]
Phase I AGS-16C3F NA Mollusk/ cyanobacterium ADC (MMAE) ENPP3 & microtubules [1+] None Cancer: Carcinoma, Renal Cell, Renal Cell Carcinoma With Clear Cell Histology, Renal Cell Carcinoma With Non-Clear Cell Histology, Renal Cell Carcinoma of Papillary Histology [Agensys & Astellas Pharma]
ASG-15ME NA Mollusk/ cyanobacterium ADC (MMAE) SLITRK6 & microtubules [1+] None Cancer: Metastatic Urothelial Cancer [Seattle Genetics]
ASG-22ME NA Mollusk/ cyanobacterium ADC (MMAE) Nectin-4 & microtubules [2+] None Cancer: Tumors; Medical Oncology; Neoplasms; Metastatic Urothelial Cancer [Seattle Genetics]
Bryostatin NA Bryozoan Macrolide
Iactone
Protein kinase C None None Cancer: Melanoma, Renal Cell Cancer, Lymphoma, Pancreatic Cancer, Fallopian Tube Cancer, Gastric Cancer, Prostate Cancer, Kidney Cancer, Lung Cancer [National Cancer Institute]
DEDN6526A NA Mollusk/ cyanobacterium ADC (MMAE) ETBR & microtubules [1+] None Cancer: Malignant Melanoma [Genentech/Roche]
DMUC5754A NA Mollusk/ cyanobacterium ADC (MMAE) Mucin 16 & microtubules None None Cancer: Ovarian Cancer, Pancreatic Cancer [Genentech/Roche]
DSTP3086S NA Mollusk/ cyanobacterium ADC (MMAE) STEAP1 & microtubules None None Cancer: Prostate Cancer [Genentech/Roche]
HuMax®-TF-ADC NA Mollusk/ cyanobacterium ADC (MMAE) Tissue Factor & microtubules [1+] None Cancer: Ovary Cancer, Cervix Cancer, Endometrium Cancer, Bladder Cancer, Prostate Cancer (CRPC), Cancer of Head and Neck (SCCHN), Esophagus Cancer, Lung Cancer (NSCLC) [GenMab]
Marizomib (Salinosporamide A; NPI-0052) NA Bacterium Beta-lactone-gamma lactam 20S proteasome [2+] None Cancer: Non-Small Cell Lung Cancer, Pancreatic Cancer, Melanoma, Lymphoma, Multiple Myeloma [Triphase]
MLN-0264 NA Mollusk/ cyanobacterium ADC (MMAE) GCC & microtublues [1+] None Cancer: Advanced Gastrointestinal Malignancies [Millennium]
PM060184 NA Sponge Polyketide Minor groove of DNA None None Cancer: Solid Tumors [Pharmamar]
SGN-CD19A NA Mollusk/
cyanobacterium
ADC (MMAF) CD19 & microtubules [2+] None Cancer: Burkitt Lymphoma, Lymphoma, Follicular, Lymphoma, Large B-Cell, Diffuse, Lymphoma, Mantle-Cell, Precursor B-cell Lymphoblastic [Seattle Genetics]
SGN-LIV1A NA Mollusk/
cyanobacterium
ADC (MMAE) LIV-1 & microtubules [1+] None Cancer: Breast Cancer [Seattle Genetics]

 

Abbreviations:
ADC: Antibody Drug Conjugate;
CD: Cluster of Differentiation;
EGFR: Epidermal Growth Factor Receptor;
ENPP3: Ectonucleotide Pyrophosphatase/Phosphodiesterase Family Member 3;
ETBR: Endothelin B Receptor;
FDA: Food and Drug Administration;
GCC: Guanylyl Cyclase C;
GPNMB: Glycoprotein nonmetastatic B;
JNK: c-Jun N-terminal protein kinases;
LIV-1: Zinc transporter SLC39A6;
MMAE: Monomethylauristatin E;
MMAF: Monomethylauristatin F;
NA: Not Available;
NaPi2b: Sodium-Dependent Phosphate Transport Protein 2b;
PSMA: Prostate-Specific Membrane Antigen;
RAC1: Ras-related C3 botulinum toxin substrate 1;
SLITRK6: SLIT and NTRK-like protein 6;
STEAP1: Anti-Six Transmembrane Epithelial Antigen of the Prostate 1


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