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PF 06650808



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Structure of PF06650808.

PF 06650808

CAS 1822383-80-1

A biologic for cancer treatment (Pfizer Inc.)

  • Originator Pfizer
  • Class Antineoplastics
  • Mechanism of Action Notch-3 receptor antagonists
  • No development reported Solid tumours
  • 24 Jun 2018 Biomarkers information updated
  • 28 Apr 2018 No recent reports of development identified for phase-I development in Solid-tumours(Late-stage disease) in USA (IV)
  • 01 Jul 2017 Pfizer completes a phase I trial in Solid tumours (Late-stage disease) in USA (IV) (NCT02129205)

Company: Pfizer

Target: Neurogenic locus notch homolog protein 3 (NOTCH3): Activation and mutation of the NOTCH signaling pathway can lead to cancer.

Disease: Cancer

Notes: PF06650808 is an antibody-drug conjugate that delivers a cytotoxic payload molecule directly to tumor cells, explained Andreas Maderna, an associate research fellow at Pfizer. The payload molecule in PF06650808 was inspired by the marine natural product dolostatin 10, which is produced by cyanobacteria consumed by a type of sea slug.


WO 2015171907

The present invention relates to stable isotopic identification of biologic products, methods of stable isotopic identification of such biologic products, and stable isotopic methods and systems for correlating biologic products to the processes by which they are made.

front page image


WO 2018045058


Rosen, L.S.; Wesolowski, R.; Gibson, B.; et al.
A Phase 1 dose escalation, safety, and pharmacokinetic study of PF-06650808, an anti-Notch3 antibody drug conjugate, in adult patients with advanced solid tumors
Eur Cancer Congr (September 25-29, Vienna) 2015, Abst 3OLBA 

Maderna, A.
Therapeutic targeting the NOTCH3 receptor with antibody drug conjugates
251st Am Chem Soc (ACS) Natl Meet (March 13-17, San Diego) 2016, Abst MEDI 262 

Hurvitz, S.A.; von Euw, E.; O’Brien, N.; et al.
Preclinical evaluation of targeting Notch-3 in breast cancer
107th Annu Meet Am Assoc Cancer Res (AACR) (April 16-20, New Orleans) 2016, Abst 1206 

Chen, J.; Geles, K.; Silva, M.; Waterhouse, R.; Ma, D.; Charati, M.; Sapra, P.; Mccarthy, T.
Evaluate the impact of conjugation on targeting capacity, pharmacokinetics and tissue distribution of antibody drug conjugate, PF-06650808, in tumor bearing mice
22nd Int Symp Radiopharm Sci (ISRS) (May 14-19, Dresden) 2017, Abst P 052 



PF 06650808

Phase 1

compound inspired by auristatins


Notch-3 receptor antagonists




PF-06650808, is currently being examined in a Ph1 clinical trial (Protocol B7501001).

Researchers are also exploring the use of Notch3 targeting. “The Notch pathway plays an important role in the growth of several solid tumours, including breast and ovarian cancer and melanoma,” explained Joerger. “In particular, Notch3 alterations such as gene amplification and upregulation are associated with poor patient survival. Research using Notch3 targeting as an innovative approach to treat solid malignancies included 27 patients unselected for Notch3 who received increasing doses of the anti-Notch3 antibody-drug conjugate PF-06650808. Responses were seen in two breast cancer patients (LBA 30). While preliminary, targeting Notch3 may become a new treatment approach in patients with selected solid tumours.”

The anti-Notch3 antibody-drug conjugate PF-06650808 is being developed by Pfizer.

  • 31 Jul 2014 Phase-I clinical trials in Solid tumours (Late-stage disease) in USA (Parenteral)
  • 30 Apr 2014 Preclinical trials in Solid tumours in USA (Parenteral)
  • 30 Apr 2014 Pfizer plans a phase I trial for Solid tumours (late-stage disease, second-line therapy or greater) in USA (NCT02129205)

251st Am Chem Soc (ACS) Natl Meet (March 13-17, San Diego) 2016, Abst MEDI 262

str1 STR2

/////////PF 06650808, PF-06650808, PF-6650808, monoclonal antibody, pfizer, phase 1, Solid tumours , Notch-3 receptor antagonists



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DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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