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▲The second TG-Bio immune technology conference in Bioogo 2021 ▲Currently, there are more than one hundred antibody drugs approved for marketing worldwide, involving 58 targets.
With the advancement of basic research and the development of pharmacy-related technologies, the regulation and control methods for the same target are becoming more and more diverse and multi-dimensional.
Looking around from the perspective of the targets of the approved antibodies, we will find that competitors are becoming more colorful, except for antibody fragments (Fab, scFv, etc.
) and antibody-like scaffold proteins (DARPin, Affibody, etc.
).
Drugs have also sprung up.
Small molecule inhibitors-the continuous expansion of small molecule kinase inhibitors that have the same target as antibodies are not new.
Gefitinib for EGFR and pyrrotinib for HER2 have already been on the market.
Most of the small molecule kinase inhibitors are multi-targets, including the classic sorafenib, sunitinib, etc.
, and their specificity is generally not high, which to a large extent leads to many clinical side effects, which is indeed worthwhile Optimization and improvement.
In addition, these small molecule inhibitors may not directly compete with antibody drugs with the same target.
For example, the HER2 inhibitor tucatinib, which was approved last year, is indicated for the treatment of HER2 positive in combination with Herceptin and capecitabine.
Breast cancer.
However, the targets of small molecule inhibitors have been expanding.
For example, the CGRPR inhibitor Ubrogepant has been on the market, becoming a favorable competitor in the migraine market.
In addition, the small molecule immune checkpoint inhibitors that have emerged in recent years are also an important force.
Taking PD-L1 as an example, the monoclonal antibodies that have been marketed include Durvalumab from AstraZeneca, Atezolizumab from Roche, and Avelumab from Merck/Pfizer.
The development of small-molecule PD-L1 inhibitors has seen gains after long-term exploration.
Hope: Compared with antibody drugs, the most important advantage of small molecule drugs is the convenience of medication.
In addition, immunogenicity and production cost can also increase the competitiveness of small molecule drugs.
Cyclic peptide drugs-the pioneer of self-contained cyclic peptide drugs, naturally recommend Bicycle Therapeutics.
Based on the artificially constructed cyclic peptide library and relying on phage display technology, the company has constructed its own early research and development system and launched a number of cyclic peptide molecules and PDC (polypeptide-drug conjugate) molecules against ADCs.
.
Currently, the company has 7 projects in the clinical stage, 4 of which are cyclic peptide drugs (BT7480, BT7455, BT7401 and THR-149), and 3 are PDC (BT1718, BT5528 and BT8009).
Among related targets, Nectin-4 has been approved for ADC drugs.
Based on the flexibility of cyclic peptide molecules, people can use chemical linkers to prepare PCD, bivalent or even multivalent cyclic peptide molecules, which can be applied to specific targets and disease scenarios.
Because the molecular weight of the cyclic peptide is very small, the derived PDC and multivalent cyclic peptide molecules are not large, and the tissue penetration is good, which can achieve aggregation at the disease site and rapid peripheral clearance.
Compared with antibody molecules and ADCs, this Class molecules theoretically have a wider therapeutic window.
In addition to Bicycle Therapeutics, there are other companies developing cyclic peptide drugs that have emerged.
For example, Protagonist Therapeutics has deployed integrin-specific cyclic peptide drugs to treat gastrointestinal inflammation, such as oral cyclic peptide PN-943 targeting integrin α4β7.
; The cyclic peptide drug zilucoplan for complement protein C5 developed by RA Pharma, which was acquired by UCB, has achieved good clinical effects and has formed a differentiated competition with antibody drugs. RNA regulation drugs-leading the future? The antibody drug track for the PCSK9 target is already crowded.
In addition to Evolocumab and Alirocumab that are already on the market, domestic Hengrui Medicine (SHR-1209), Cinda Biotech (tafolecimab), Junshi Biotech (JS002), etc.
have all been deployed.
There is not much room for latecomers both at home and abroad.
.
Novartis' inclisiran is a small interfering RNA (siRNA) drug administered by subcutaneous injection, which reduces protein expression by degrading the mRNA of PCSK9.
Clinical data shows that the drug can be injected once every 6 months, which is very convenient.
In addition to PCSK9, there are also RNA-regulated drugs under development for the target of AGPTL3, such as the antisense nucleotide molecule Vupanorsen jointly developed by Ionis and Pfizer.
Currently, biotechnology companies represented by Alnylam and Ionis have extensively deployed RNA interference drugs.
The bottleneck of the entire field is the drug delivery carrier.
If continuous improvement in this area, the target will be further expanded, and the market for related drugs will also be further expanded.
PCSK9-Fancy competition As mentioned above, the research and development of PCSK9 is already crowded.
But a careful investigation reveals that the competition is quite multi-dimensional.
The first is antibody drugs.
Two are already on the market and many are under development.
The dimension of monoclonal antibodies is close to saturation.
The second is siRNA drugs.
Novartis' inclisiran has been listed in the EU, and it is only a matter of time before it is approved by the FDA.
The administration method of subcutaneous injection once every 6 months is extremely convenient, and it is believed that it will be favored by the majority of patients.
There are also small molecule drugs, and there are currently two categories: one category is the oral small molecule CVI-LM001 of Siweier Medicine, which can reduce the expression of the PCSK9 gene; the other category is a small molecule inhibitor that directly binds to the PCSK9 protein.
Foreign companies such as Dogma and domestic Xinlitai have already made arrangements. PCSK9 is just a representative.
In the future, there will be more targets showing the competition of multi-dimensional treatment methods.
The editor concludes that the replacement of antibody drugs by small molecules has become an intentional or unintentional trend.
In addition to the targets that have been marketed for antibodies such as PD-L1, CGRPR, Nectin-4, etc.
, there are no approved targets for antibody drugs.
, Such as CD73, etc.
, the research and development progress of small molecule drugs is not lagging behind.
The advantages of small-molecule drugs are mainly reflected in the convenience and cost control of oral medication.
If safety (off-target effects) is not delayed, it will be promising.
The advantages of RNA-regulated drugs (mainly siRNA) are reflected in greatly reducing the frequency of medication, which not only significantly improves the convenience of medication, but also reduces the cost of medication.
The main shortcomings are that the target is limited (the reason for the targeting and efficiency of drug delivery), and the second is that the long-term safety in vivo has yet to be demonstrated.
Appendix: Copyright statements of antibody drugs approved for marketing and other types of drugs with the same target are welcome to share.
Any other media or website that needs to reprint or quote the copyrighted content of this website must be authorized and marked "Reprinted from: Biopharmaceutical Editor" in a prominent position.
With the advancement of basic research and the development of pharmacy-related technologies, the regulation and control methods for the same target are becoming more and more diverse and multi-dimensional.
Looking around from the perspective of the targets of the approved antibodies, we will find that competitors are becoming more colorful, except for antibody fragments (Fab, scFv, etc.
) and antibody-like scaffold proteins (DARPin, Affibody, etc.
).
Drugs have also sprung up.
Small molecule inhibitors-the continuous expansion of small molecule kinase inhibitors that have the same target as antibodies are not new.
Gefitinib for EGFR and pyrrotinib for HER2 have already been on the market.
Most of the small molecule kinase inhibitors are multi-targets, including the classic sorafenib, sunitinib, etc.
, and their specificity is generally not high, which to a large extent leads to many clinical side effects, which is indeed worthwhile Optimization and improvement.
In addition, these small molecule inhibitors may not directly compete with antibody drugs with the same target.
For example, the HER2 inhibitor tucatinib, which was approved last year, is indicated for the treatment of HER2 positive in combination with Herceptin and capecitabine.
Breast cancer.
However, the targets of small molecule inhibitors have been expanding.
For example, the CGRPR inhibitor Ubrogepant has been on the market, becoming a favorable competitor in the migraine market.
In addition, the small molecule immune checkpoint inhibitors that have emerged in recent years are also an important force.
Taking PD-L1 as an example, the monoclonal antibodies that have been marketed include Durvalumab from AstraZeneca, Atezolizumab from Roche, and Avelumab from Merck/Pfizer.
The development of small-molecule PD-L1 inhibitors has seen gains after long-term exploration.
Hope: Compared with antibody drugs, the most important advantage of small molecule drugs is the convenience of medication.
In addition, immunogenicity and production cost can also increase the competitiveness of small molecule drugs.
Cyclic peptide drugs-the pioneer of self-contained cyclic peptide drugs, naturally recommend Bicycle Therapeutics.
Based on the artificially constructed cyclic peptide library and relying on phage display technology, the company has constructed its own early research and development system and launched a number of cyclic peptide molecules and PDC (polypeptide-drug conjugate) molecules against ADCs.
.
Currently, the company has 7 projects in the clinical stage, 4 of which are cyclic peptide drugs (BT7480, BT7455, BT7401 and THR-149), and 3 are PDC (BT1718, BT5528 and BT8009).
Among related targets, Nectin-4 has been approved for ADC drugs.
Based on the flexibility of cyclic peptide molecules, people can use chemical linkers to prepare PCD, bivalent or even multivalent cyclic peptide molecules, which can be applied to specific targets and disease scenarios.
Because the molecular weight of the cyclic peptide is very small, the derived PDC and multivalent cyclic peptide molecules are not large, and the tissue penetration is good, which can achieve aggregation at the disease site and rapid peripheral clearance.
Compared with antibody molecules and ADCs, this Class molecules theoretically have a wider therapeutic window.
In addition to Bicycle Therapeutics, there are other companies developing cyclic peptide drugs that have emerged.
For example, Protagonist Therapeutics has deployed integrin-specific cyclic peptide drugs to treat gastrointestinal inflammation, such as oral cyclic peptide PN-943 targeting integrin α4β7.
; The cyclic peptide drug zilucoplan for complement protein C5 developed by RA Pharma, which was acquired by UCB, has achieved good clinical effects and has formed a differentiated competition with antibody drugs. RNA regulation drugs-leading the future? The antibody drug track for the PCSK9 target is already crowded.
In addition to Evolocumab and Alirocumab that are already on the market, domestic Hengrui Medicine (SHR-1209), Cinda Biotech (tafolecimab), Junshi Biotech (JS002), etc.
have all been deployed.
There is not much room for latecomers both at home and abroad.
.
Novartis' inclisiran is a small interfering RNA (siRNA) drug administered by subcutaneous injection, which reduces protein expression by degrading the mRNA of PCSK9.
Clinical data shows that the drug can be injected once every 6 months, which is very convenient.
In addition to PCSK9, there are also RNA-regulated drugs under development for the target of AGPTL3, such as the antisense nucleotide molecule Vupanorsen jointly developed by Ionis and Pfizer.
Currently, biotechnology companies represented by Alnylam and Ionis have extensively deployed RNA interference drugs.
The bottleneck of the entire field is the drug delivery carrier.
If continuous improvement in this area, the target will be further expanded, and the market for related drugs will also be further expanded.
PCSK9-Fancy competition As mentioned above, the research and development of PCSK9 is already crowded.
But a careful investigation reveals that the competition is quite multi-dimensional.
The first is antibody drugs.
Two are already on the market and many are under development.
The dimension of monoclonal antibodies is close to saturation.
The second is siRNA drugs.
Novartis' inclisiran has been listed in the EU, and it is only a matter of time before it is approved by the FDA.
The administration method of subcutaneous injection once every 6 months is extremely convenient, and it is believed that it will be favored by the majority of patients.
There are also small molecule drugs, and there are currently two categories: one category is the oral small molecule CVI-LM001 of Siweier Medicine, which can reduce the expression of the PCSK9 gene; the other category is a small molecule inhibitor that directly binds to the PCSK9 protein.
Foreign companies such as Dogma and domestic Xinlitai have already made arrangements. PCSK9 is just a representative.
In the future, there will be more targets showing the competition of multi-dimensional treatment methods.
The editor concludes that the replacement of antibody drugs by small molecules has become an intentional or unintentional trend.
In addition to the targets that have been marketed for antibodies such as PD-L1, CGRPR, Nectin-4, etc.
, there are no approved targets for antibody drugs.
, Such as CD73, etc.
, the research and development progress of small molecule drugs is not lagging behind.
The advantages of small-molecule drugs are mainly reflected in the convenience and cost control of oral medication.
If safety (off-target effects) is not delayed, it will be promising.
The advantages of RNA-regulated drugs (mainly siRNA) are reflected in greatly reducing the frequency of medication, which not only significantly improves the convenience of medication, but also reduces the cost of medication.
The main shortcomings are that the target is limited (the reason for the targeting and efficiency of drug delivery), and the second is that the long-term safety in vivo has yet to be demonstrated.
Appendix: Copyright statements of antibody drugs approved for marketing and other types of drugs with the same target are welcome to share.
Any other media or website that needs to reprint or quote the copyrighted content of this website must be authorized and marked "Reprinted from: Biopharmaceutical Editor" in a prominent position.
