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Afatinib (BIBW2992)

Rating: Māhele:

ʻO ka pauma Afatinib, kūʻai ʻia ma lalo o ka inoa inoa Gilotrif i waena o nā mea ʻē aʻe, kahi lāʻau i hoʻohana ʻia e mālama ai i ka maʻi liʻiliʻi liʻiliʻi liʻiliʻi (NSCLC). Pili ia i ka ʻohana inhibitor tyrosine kinase o nā lāʻau. Lawe ʻia e ka waha.

Product Description

Nā ʻano kikoʻī

Product Name Paukū Afatinib (BIBW2992)
Kāleka CAS 850140-73-7
Ka Lā Molecular C32H33ClFN5O11
Kaumaha Kaumaha 718.09
'O Synonyms 850140-73-7;

BIBW-2992;

BIBW 2992;

BIBW2992. Afatinib pauma dimaleate;

Keʻano ʻO ka'ōmaʻomaʻo māmā
Ka mālama a me ka lima lima Maloʻo, ʻeleʻele a ma 0 - 4 C no ka wā pōkole (mau lā a i mau pule) a i ʻole -20 C no ka wā lōʻihi (mau mahina i mau makahiki).

 

Hōʻike Powder Afatinib

ʻO ka pauma Afatinib, kūʻai ʻia ma lalo o ka inoa ʻo Gilotrif i waena o nā mea ʻē aʻe, kahi lāʻau i hoʻohana ʻia e mālama ai i ka maʻi liʻiliʻi liʻiliʻi liʻiliʻi (NSCLC). Pili ia i ka ʻohana inhibitor tyrosine kinase o nā lāʻau. Lawe ʻia e ka waha. Hoʻohana nui ʻia ia e mālama i nā hihia o NSCLC e mālama i nā hoʻololi i ka ʻenemi ulu ulu epidermal (EGFR).

ʻO ka pauma Afatinib (BIBW2992), kahi mea pāpā i hiki ʻole ke hoʻihoʻi ʻia o ka ʻohana ErbB o nā kinase tyrosine, i hōʻike ʻia e kāohi i ka phosphorylation i hoʻokomo ʻia e EGF o EGFR a me ka hoʻonui ʻana o ka pūnaewele i nā ʻano laina EGFR-overexpressing a me HER2 e hōʻike ana e like me A431, NIH-3T3 -HER2, NCI-N87 a me BT-474.

Ua hoʻohana nui ʻia ka mea i loko o nā ʻano holoholona like ʻole e hoʻopaʻa i ke kuleana o EGFR / HER2. ʻO ka lawelawe ʻana i ka waha o ka pauuma afatinib ka mea i kāohi i ka ulu ʻana o ka maʻi ʻaʻai a me ke ola ʻana a kāohi i ka hoʻihoʻi ʻia o ka tumo ma xenograft a me nā ʻōnaehana maʻi ʻaʻa transgenic Hoʻohui ʻia, ʻike ʻia ka paukū afatinib ma ke ʻano he EGFR blocker i ʻae ʻia no ka mālama ʻana i nā mea maʻi me ka maʻi ʻaʻaʻa nonsmall mutated EGFR

 

ʻO Afatinib Powder Mekanika o ka Hana

E like me ka lapatinib a me ka neratinib, ʻo ka pauma afatinib kahi mea hoʻopōpō kinase protein i hiki ʻole hoʻi ke kāohi i ka mea ulu kanaka epidermal ulu 2 (Her2) a me nā ʻepekema ulu ulu epidermal (EGFR) kinases

ʻAʻole hana wale ka paukū Afatinib e kūʻē i nā hoʻololi EGFR i hoʻolālā ʻia e nā hanauna mua tyrosine-kinase (TKI) e like me erlotinib a i ʻole gefitinib, akā e kūʻē pū ana hoʻi i nā loli liʻiliʻi i kū ʻole i kēia mau lāʻau.

Eia nō naʻe, ʻaʻole ia e kūʻē i ka mutation T790M e koi pinepine ai i nā lāʻau ʻekolu e like me osimertinib. Ma muli o kāna hana hou aku e kūʻē iā Her2, ʻimi ʻia nei no ka maʻi ʻaʻai umauma a me nā maʻi ʻino ʻē aʻe EGFR a me Her2..

 

Noi Afatinib Powder

ʻO ka pauma Afatinib kahi ʻohana anilino-quinazoline i loaʻa i ka waha a me ka mea hōʻemi o ka receptor tyrosine kinase (RTK) ʻepekema ulu ulu (ErbB; EGFR) ʻohana, me ka antineoplastic hana.

ʻO ka pauma Afatinib kekahi mea bioavailable oral receptor tyrosine kinase (RTK) mea kāohi me ka hana antineoplastic hiki. Hoʻopaʻa ʻo EGFR / HER2 tyrosine kinase mea hoʻopaʻa iā BIBW 2992 i ka a kāohi i nā mea ulu ulu epidermal kanaka 1 a me 2 (EGFR-1; HER2), a he hopena paha ia i ka pāpā ʻana i ka ulu ulu a me angiogenesis. ʻO EGFR / HER2 nā RTK e pili ana i ka ʻohana super EGFR; pāʻani nā mea ʻelua i ka nui o ka ulu ʻana o ka cell tumor a me ka vascularization o ka tumora a ua hōʻike ʻia i loko o nā ʻano pūnaeho maʻi ʻaʻai.

ʻAe ʻia ka paukū ʻo Afatinib i ka hapa nui o ka honua (e like me ʻAmelika Hui Pū ʻIa, Kanada, ke Aupuni Hui Pū ʻia a me ʻAukekulia) no ka mālama ʻana i ka carastoma baga liʻiliʻi liʻiliʻi liʻiliʻi (NSCLC), hoʻomohala ʻia e Boehringer Ingelheim. Hana ia ma ke ʻano he mea hōʻoki angiokinase.

 

Nā hopena ʻaoʻao ʻo Afatinib Powder & Warning

ʻO nā hopena ʻē aʻe i maʻa mau (e ʻike ʻia ma mua o 30%) no nā mea maʻi e lawe ana i ka pauma afatinib:

▪ Pohā

▪ Hū ka huehue (ka hui o nā ʻili i like me ka huehue)

▪ Wela ka waha

▪ Paronychia (maʻi o nā kui)

▪ waha maloo

 

ʻO kēia nā hopena ʻē aʻe i ʻike pinepine ʻia (e loaʻa ana ma 10-29%) no nā mea maʻi e loaʻa ana i ka pauma afatinib:

▪ Hoʻoemi i ka makemake

▪ Kāwili

▪ Ka hoʻēmi kino

▪ Kahe ka ihu

▪ Cystitis (maʻi ʻaʻai)

▪ Cheilitis (pehu o nā lehelehe)

▪ Fiva

▪ Hypokalemia (potassium haʻahaʻa)

▪ Conjunctivitis (maka poni)

▪ Rhinorrhea (ihu ihu)

▪ Nā ʻenekia ate kiʻekiʻe

ʻAʻole i helu ʻia nā hopena ʻaoʻao āpau ma luna. Kekahi mau mea kākaʻikahi (e hana ʻia ma lalo o 10 pākēneka o nā maʻi) ʻaʻole i helu ʻia ma aneʻi. Hoʻomaopopo mau i kāu mea mālama ola inā ʻike ʻoe i nā ʻōuli maʻamau.

 

Nā mea nui e hoʻomanaʻo e pili ana i nā hopena ʻaoʻao o ka pauma afatinib:

▪ ʻAʻole ʻike ka hapa nui o nā poʻe i nā hopena ʻaoʻao āpau afatinib i helu ʻia.

▪ Kuhi pinepine ʻia nā hopena ʻaoʻao ʻo Afatinib e pili ana i ka hoʻomaka, ka lōʻihi, a me ke koʻikoʻi.

▪ ʻAneʻane hiki ke hoʻohuli i nā hopena ʻaoʻao ʻo Afatinib a e hele aku ma hope o ka pau ʻana o ka lāʻau.

▪ Hiki ke mālama ʻia nā hopena ʻaoʻao ʻo Afatinib. Nui a hewahewa nā koho e hoʻoliʻiliʻi a pale i nā hopena ʻaoʻao o ka pauma afatinib.

 

Reference

[1] Prim N, Fore M, Mennecier B. [Afatinib pauka (BIBW 2992).]. ʻO Rev Pneumol Clin. 2014 Mei 27. pii: S0761-8417 (14) 00047-9. hana: 10.1016 / j.pneumo.2014.03.002. [Epub ma mua o ka paʻi] Nānā. Palani. ʻO PubMed PMID: 24878189.

[2] DʻArcangelo M, Hirsch FR. Pono pono a me ka hoʻohālikelike o ka pauma afatinib i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi. ʻO Biologics. 2014 ʻApel 23; 8: 183-92. hana: 10.2147 / BTT.S40567. eCollection 2014. Loiloi. PubMed PMID: 24790411; PubMed Central PMCID: PMC4003149.

[3] Bowles DW, Weickhardt A, Jimeno A. Afatinib pauma no ka mālama ʻana i nā mea maʻi me ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi liʻiliʻi ʻo EGFR. Nā lāʻau i kēia lā (Barc). 2013 Sep; 49 (9): 523-35. hana: 10.1358 / kiko.2013.49.9.2016610. Loiloi. PubMed PMID: 24086949.

[4] KÃÃhler J, Schuler M. Afatinib pauka, erlotinib a me gefitinib i ka lalani mua o EGFR mutation-positive lung adenocarcinoma: he loiloi. Onkologie. 2013; 36 (9): 510-8. hana: 10.1159 / 000354627. Epub 2013 Aug 19. Loiloi. PMID PubMed: 24051929.

[5] Yap TA, Popat S. ʻO ke kuleana o ka paukū afatinib i ka mālama ʻana i ka carcinoma māmā liʻiliʻi liʻiliʻi ʻole. ʻO ka loea ʻo Opin Drug Metab Toxicol. 2013 Nov; 9 (11): 1529-39. hana: 10.1517 / 17425255.2013.832755. Epub 2013 Aug 28. Loiloi. ʻO PubMed PMID: 23985030.

[6] Dungo RT, Keating GM. Paukū Afatinib: ʻae ʻia ka honua mua. Nā lāʻau. 2013 Sep; 73 (13): 1503-15. hana: 10.1007 / s40265-013-0111-6. Loiloi. ʻO PubMed PMID: 23982599.

[7] Minkovsky N, Berezov A (Kekemapa 2008). "BIBW-2992, kahi pālua receptor tyrosine kinase inhibitor no ka mālama ʻana i nā tumors paʻa". ʻO ka manaʻo o kēia manawa i nā lāʻau lapaʻau noiʻi. 9 (12): 1336–46. PMID 19037840

[8] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, et al. (ʻAukake 2008). "BIBW2992, kahi mea hoʻohuli EGFR / HER2 i hiki ʻole ke hoʻoliʻiliʻi maikaʻi loa i nā mana maʻi ʻaʻai maʻi preclinical". ʻO Oncogene. 27 (34): 4702-11. hana: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761.


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