本報告已在2011年07月19日停止出版。
長期進行臨床實驗的血管標的藥劑（VTA），屬於中和微管蛋白細胞骨架的小分子藥物。2004年在傳統研究上有顯著突破的企業有數家，邁入第II期的個案有2件、第I期的個案有2件；另外發表從2005年開始進行新研發的企業也有數家，邁向第III期的替補藥也為數不少。
近來在醫藥及生物技術領域的調查分析上富有績效的瑞典調查公司 BioSeeker Group ，調查與分析血管標的藥劑（VTA）市場，並有系統地出版綜合報告書 "Vascular Targeting Agents: Emerging Competitors" 。
此報告書在下面的內容裡，針對血管標的藥劑（VTA）的最新開發狀況，進行詳盡地探討。
此商品為英文報告書 Cancer Highlights 的其中一部分。
- 概要
- 多數處於臨床階段的血管標的藥劑
- 新臨床企劃的 Vanguard VTA
- VTA 與抗血管新生藥劑的組合
- 使微血管不安定的非 Combretastatins 劑
- 隱藏成為 VTA 可能性的微小管作用藥（AMD）
- 當作傳送工具的單株抗體
- 內皮細胞的獨特性連接的標的化
- 陽離子型微脂粒的加封化
- 圖表
Abstract
In this issue of Cancer Highlights, BioSeeker Group analyzes the progress made for vascular
targeting agents (VTA). You will receive an update on the most recent advances made for vascular
targeting agents that are now entering an exciting stage of development. In only a few years time
the number of candidates has been doubled, expanding from a handful of drugs to more than twenty.
Several of these have entered clinical evaluation. Earlier and most talked of candidates still
remain at the top. However, the list of emerging competitors is growing and at least seven new VTAs
have recently entered clinic settings. Not so far away, there are also several vascular targeting
agents that are on the brim of initiating Phase I trials.
Vascular targeting agents with the longest clinical experience are the small molecular drugs that
mediate their action on the tubulin cytoskeleton. In review of 2004, several companies have
announced progression on existing studies. In addition two new Phase II trials and two new Phase I
trials have been launched. Several companies have made announcements of plans to initiate new trials
during 2005. A few candidates are now in planning for Phase III trial studies.
Despite compelling preclinical data, the conjugated antibodies have been delayed in comparison to
the small molecule approaches. Trial initiation is thus long overdue for many. We have devoted an
entire section of this Highlight to "Monoclonal antibodies as Delivery Vehicles" where the
progression for several of the most important conjugated antibodies is outlined. One of these
antibodies is already in Phase I and for which plans are laid for Phase II during 2005.
The close relation between vascular targeting and anti-angiogenesis also make it possible for new
competitors to enter the scene in near future. One relative large company, with a strong anti-angiogenesis
antibody portfolio, has already announced to hold a vascular targeting antibody in early stage of
development.
In total BioSeeker Group has identified 26 different therapies that have been developed utilizing
vascular targeting strategies:
3G4, ABT-751, AVE8062A, AZD4440, BCH-19746, BCH-23541, CA4P, DMXAA, E4G10, EndoTAG-1, EndoTAG-2,
Exherin, ILX-651, MLN2704, MLN591, MLN591RL, MN-029, MX116407, NPI-2358, OXi4503, OXi6197, OXi8009,
Tarvacin, TZT-1027, VEGF121/rGel, ZD6126
Table of Contents
- Table of Contents2
- BSG General Working Model & Methodology3
- Introduction5
- More Vascular Targeting Drugs in Clinical Trial8
- Table 1 Summary of VTA agents under development9
- The Vanguard VTA in New Clinical Programs10
- Combination of VTAs and antiangiogenic agents18
- The Non-Combretastatins Agents that Destabilize Microtubules21
- Antimicrotubule Agents with Vascular Targeting Potential27
- Monoclonal Antibodies as Delivery Vehicles30
- Targeting Endothelial Cell-Specific Adhesion37
- Encapsulation in cationic liposomes40
- Disclaimer42
- Liability42
- Completeness42
- Appendix43
- Table 2. CA4P Near Term Progress43
- Table 3. Oxi 4503 Near Term Progress47
- Table 4. AVE8062A Near Term Progress48
- Table 5. ZD6126 Near Term Progress49
- Table 6. DMXAA Near Term Progress52
- Table 7. ABT-751 Near Term Progress55
- Table 8. MN-029 Near Term Progress56
- Table 9. MX116407 Near Term Progress56
- Table 10. NPI-2358 Near Term Progress57
- Table 11. TZT-1027 Near Term Progress58
- Table 12. ILX-651 Near Term Progress59
- Table 13. Peregrines VTA and APT platforms Near Term Progress60
- Table 14. VEGF121/rGelonin Near Term Progress63
- Table 15. MLN2704 Near Term Progress64
- Table 16. Adherexs cadherin platform Near Term Progress66
- Table 17. E4G10 Near Term Progress67
- Table 18. EndoTAG-1 Near Term Progress68
