Protein kinase C (PKC) is a family of phospholipid-dependent serine/threonine kinases. PKCs are involved in multiple signal transduction systems that control cell proliferation, differentiation, survival, invasion, migration, and apoptosis. PKC inhibitors act by inhibiting DAG (C1 domain-binding inhibitors), or by inhibiting ATP (C3 domain-binding inhibitors), or by inhibiting the substrate (C4 domain-binding inhibitors), whereas the PKC activators act by binding to the C1 domain. PKC inhibitors have been marketed for liver cancer, renal-cell carcinoma, thyroid cancer, and actinic keratosis. PKCs are also being targeted for neurological diseases such as Alzheimer’s disease, cardiovascular diseases such as heart failure, and infections. Takeda Pharmaceutical, Exelixis, Novartis, Mirati Therapeutics, Eli Lilly & Company, Pfizer, and Roche are some of the major players in the protein kinase C inhibitors market.
Key Market Developments:
- In Nov 2021, Qurien Therapeutics and Merck & Co entered into a collaboration agreement for q-701, a proto-oncogene protein c-mer inhibitor in the USA and South Korea for solid tumors.
- In Dec 2022, Exelixis received patent protection for Zanzalintinib in the USA.
- In Feb 2023, Atossa Therapeutics received a patent from the US PTO for (Z)-Endoxifen encapsulated in an enteric capsule.
Approved Drug Molecules and Brand Names for Protein Kinase C Modulators:
- Cabometyx (Cabozantinib tablet)
- Picato Gel (Ingenol mebutate)
Drugs under the Pipeline for Protein Kinase C Modulators:
- Rydapt (Midostaurin)
- Kinenza (Enzastaurin)
- Sitravatinib (MGCD516)
- Sotrastaurin (AEB071)
- Arxxant (Ruboxistaurin oral)
- Ningetinib (CT053PTSA)
- Tigilanol tiglate (EBC-46)
- MS-553
- Zanzalintinib (XL092)
- MRX2843
- Zonalta (Z-Endoxifen hydrochloride)
- Bryostatin 1 (NSC 339555)
- Darovasertib (IDE196)
- KAI-1678
- ONO-7475
- PCUR-101
- Q702
- Tetradecanoylphorbol acetate (PD-616)
- AHT956
- AR-13503
- CC-90005
- EXS4318
- INCB81776
- PF-07265807
- RXDX-106
- SKI-G-801
- Ruboxistaurin topical (DBI-102)
Clinical Activity and Developments of Protein Kinase C Modulators:
Currently, there are about 29 drug products in protein kinase C inhibitor, including 2 approved drug molecules, and others are in clinical trial phases.
- In Feb 2023, Ming Sight-Relin Pharmaceutical initiated a phase-I/II clinical trial in chronic lymphocytic leukemia and non-hodgkin’s lymphoma in China for MS-553, a protein kinase C beta inhibitor.
- In Mar 2023, BeiGene completed a phase-I/II trial in gastric cancer and liver cancer for Sitravatinib in China.
- In Apr 2023, QBiotics conducted phase-II clinical trials in the USA in soft tissue sarcoma for Tigilanol tiglate.
|
Molecule Name |
Number of Studies |
|
Rydapt (Midostaurin) |
58 |
|
Kinenza (Enzastaurin) |
55 |
|
Sitravatinib (MGCD516) |
37 |
|
Sotrastaurin (AEB071) |
23 |
|
Arxxant (Ruboxistaurin oral) |
15 |
|
Ningetinib (CT053PTSA) |
7 |
|
Tigilanol tiglate (EBC-46) |
7 |
|
MS-553 |
5 |
|
Zanzalintinib (XL092) |
5 |
|
MRX2843 |
4 |
|
Zonalta (Z-Endoxifen hydrochloride) |
4 |
|
Bryostatin 1 (NSC 339555) |
4 |
|
Darovasertib (IDE196) |
4 |
|
KAI-1678 |
3 |
|
ONO-7475 |
2 |
|
PCUR-101 |
2 |
|
Q702 |
2 |
|
Tetradecanoylphorbol acetate (PD-616) |
2 |
|
AHT956 |
1 |
|
AR-13503 |
1 |
|
CC-90005 |
1 |
|
EXS4318 |
1 |
|
INCB81776 |
1 |
|
PF-07265807 |
1 |
|
RXDX-106 |
1 |
|
SKI-G-801 |
1 |
|
Ruboxistaurin topical (DBI-102) |
1 |
Target Indication Analysis of Protein Kinase C Modulators
Cabozantinib is marketed for liver cancer, renal cell carcinoma, and thyroid cancer, and is in phase-III for non-small cell lung cancer and prostate cancer. Ingenol mebutate is used in the treatment of actinic keratosis. Enzastaurin is in phase-III for diffuse large B cell lymphoma, Ehlers-Danlos syndrome, glioblastoma. Sitravatinib is in phase-III for non-small cell lung cancer, ovarian cancer and renal cell carcinoma, and in phase-II/III for solid tumors. Ruboxistaurin is in phase-II for hyperpigmentation, melanosis, and skin disorders. Zanzalintinib is in phase-III for colorectal cancer and renal cell carcinoma.
Regional Analysis of Protein Kinase C Modulators
Protein Kinase C Modulators Market
Exelixis’s Cabometyx (Cabozantinib) had a total sale of US$ 1,376 in the USA in 2022, which was an increase from the sales of US$ 1,054 million in 2021 and the company will see all of the patent expiration for Cabometyx by 2033. LEO Labs Picato’s (Ingenol mebutate) patent for the treatment of actinic keratosis will expire in May 2033. Cancer is one of the leading causes of mortality globally. According to the World Health Organization, China had the highest new cases of leukemia (85,404), followed by the USA (61,252), and India (48,419) in 2020. In the case of liver cancer, China had 4,10,038 new cases, followed by Japan (45,663) and the USA (42,284) in 2020. For thyroid cancer, China had the highest number of new cases (2,21,093), followed by the USA (52,912).
Latin America
Europe
Asia Pacific
Middle East
North America
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Frequently Asked Questions
Cabometyx (Cabozantinib tablet), Picato Gel (Ingenol mebutate) are the approved protein kinase C modulators in the market.
Takeda Pharmaceutical, Exelixis, Novartis, Mirati Therapeutics, Eli Lilly & Company, Pfizer, and Roche are some of the major players in the protein kinase C inhibitors market.
Major indications for liver cancer, renal-cell carcinoma, thyroid cancer, and actinic keratosis.
There are more than 20 molecules in the clinical development for protein kinase C modulators.
- Takeda Pharmaceutical
- Exelixis
- Novartis
- Mirati Therapeutics
- Eli Lilly & Company
- HEC Pharma
- MingSight Pharma
- Intas Pharmaceutical
- Ideaya Bioscience
- Amgen
- Ono Pharma
- Aerie Pharma
- BMS
- Incyte Corporation
- Pfizer
- Roche