Substance P: Difference between revisions

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==Drugs that target Substance P==

Due to its association with largely negative phenomena (pain, stress responses ~~and~~ affective disorders, vomiting), drug development has been focused on Substance P antagonists. Since SP is a high-affinity ligand for the NK1 receptor, NK1 receptor antagonists were the first to be developed. However SP also binds to NK2 and NK3 receptors, and related neuropeptides have higher affinity for these receptors, so development of antagonists for these receptors has also been pursued. There are a number of NK1 antagonists attested in the medical literature, but few of them are in use. They include:

Due to its association with largely negative phenomena (pain, stress responses, affective disorders, and vomiting), drug development has been focused on Substance P antagonists. Since SP is a high-affinity ligand for the NK1 receptor, NK1 receptor antagonists were the first to be developed. However, SP also binds to NK2 and NK3 receptors and related neuropeptides have higher affinity for these receptors, so development of antagonists for these receptors has also been pursued. There are a number of NK1 antagonists attested in the medical literature, but few of them are in use. They include:

* Aprepitant, a failed antidepressant that ~~succeded~~ in clinical trials for chemotherapy-induced vomiting and nausea (CIVN) and was FDA approved for treating CIVN in 2004.

* Aprepitant is a failed antidepressant that succeeded in clinical trials for chemotherapy-induced vomiting and nausea (CIVN) and was FDA approved for treating CIVN in 2004.

* Netupitant, FDA approved for CIVN in a combination product with another antiemetic, palonosetron, in 2014.

* Netupitant is FDA approved for CIVN in a combination product with another antiemetic, palonosetron, in 2014.

* CP-99,994, which reached phase II clinical trials for dental pain. It was able to replicate the effect of ibuprofen on postoperative dental pain,<ref>http://onlinelibrary.wiley.com/doi/10.1016/S0009-9236(98)90140-0/abstract</ref> but trials were discontinued due to poor oral bioavailability.

* CP-99,994 which reached phase II clinical trials for dental pain. It was able to replicate the effect of ibuprofen on postoperative dental pain,<ref>http://onlinelibrary.wiley.com/doi/10.1016/S0009-9236(98)90140-0/abstract</ref> but trials were discontinued due to poor oral bioavailability.

* Maropitant (brand name '''Cerenia'''), FDA approved for treatment and prevention of vomiting in cats and dogs.<ref>https://vetlabel.com/lib/vet/meds/cerenia-1/</ref>

* Maropitant (brand name '''Cerenia''') is FDA approved for treatment and prevention of vomiting in cats and dogs.<ref>https://vetlabel.com/lib/vet/meds/cerenia-1/</ref>

* Vestipitant, currently under development for use against, among other things, insomnia.<ref>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3825431/</ref>

* Vestipitant is currently under development for use against, among other things, insomnia.<ref>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3825431/</ref>

* Fosaprepitant, a [[prodrug]] for aprepitant.

* Fosaprepitant is a [[prodrug]] for aprepitant.

==See also==

@@ Line 57: / Line 57: @@
 ==Drugs that target Substance P==
-Due to its association with largely negative phenomena (pain, stress responses and affective disorders, vomiting), drug development has been focused on Substance P antagonists. Since SP is a high-affinity ligand for the NK1 receptor, NK1 receptor antagonists were the first to be developed. However SP also binds to NK2 and NK3 receptors, and related neuropeptides have higher affinity for these receptors, so development of antagonists for these receptors has also been pursued. There are a number of NK1 antagonists attested in the medical literature, but few of them are in use. They include:
+Due to its association with largely negative phenomena (pain, stress responses, affective disorders, and vomiting), drug development has been focused on Substance P antagonists. Since SP is a high-affinity ligand for the NK1 receptor, NK1 receptor antagonists were the first to be developed. However, SP also binds to NK2 and NK3 receptors and related neuropeptides have higher affinity for these receptors, so development of antagonists for these receptors has also been pursued. There are a number of NK1 antagonists attested in the medical literature, but few of them are in use. They include:
-* Aprepitant, a failed antidepressant that succeded in clinical trials for chemotherapy-induced vomiting and nausea (CIVN) and was FDA approved for treating CIVN in 2004.
+* Aprepitant is a failed antidepressant that succeeded in clinical trials for chemotherapy-induced vomiting and nausea (CIVN) and was FDA approved for treating CIVN in 2004.
-* Netupitant, FDA approved for CIVN in a combination product with another antiemetic, palonosetron, in 2014.
+* Netupitant is FDA approved for CIVN in a combination product with another antiemetic, palonosetron, in 2014.
-* CP-99,994, which reached phase II clinical trials for dental pain. It was able to replicate the effect of ibuprofen on postoperative dental pain,<ref>http://onlinelibrary.wiley.com/doi/10.1016/S0009-9236(98)90140-0/abstract</ref> but trials were discontinued due to poor oral bioavailability.
+* CP-99,994 which reached phase II clinical trials for dental pain. It was able to replicate the effect of ibuprofen on postoperative dental pain,<ref>http://onlinelibrary.wiley.com/doi/10.1016/S0009-9236(98)90140-0/abstract</ref> but trials were discontinued due to poor oral bioavailability.
-* Maropitant (brand name '''Cerenia'''), FDA approved for treatment and prevention of vomiting in cats and dogs.<ref>https://vetlabel.com/lib/vet/meds/cerenia-1/</ref>
+* Maropitant (brand name '''Cerenia''') is FDA approved for treatment and prevention of vomiting in cats and dogs.<ref>https://vetlabel.com/lib/vet/meds/cerenia-1/</ref>
-* Vestipitant, currently under development for use against, among other things, insomnia.<ref>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3825431/</ref>
+* Vestipitant is currently under development for use against, among other things, insomnia.<ref>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3825431/</ref>
-* Fosaprepitant, a [[prodrug]] for aprepitant.
+* Fosaprepitant is a [[prodrug]] for aprepitant.
 ==See also==